Glucagon

Areas of active research — not promised effects

Each tag links to other compounds with research into that goal. Research use only: these are areas of study, not human-use claims.

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Glucagon rDNA origin is an approved Rx-only prescription medicine in the United States. Multiple brand-name products are FDA-approved: GlucaGen HypoKit (Novo Nordisk), Gvoke (Xeris; HypoPen, prefilled syringe, and VialDx), and Baqsimi (Eli Lilly; intranasal powder). Gvoke VialDx was approved May 14, 2025. It may be legally dispensed by licensed pharmacies with a valid prescription.

Confirmed high-severity market-integrity event (enforcement / recall / counterfeit)

Transparent blend · bci-1.0 · never paid-placement

Primary name

Glucagon

Origin

Glucagon is a 29-amino acid peptide hormone produced and secreted by the alpha cells of the pancreatic islets of Langerhans. It is a member of the glucagon/secretin superfamily and functions as the primary counterregulatory hormone to insulin. Therapeutic glucagon is produced by recombinant DNA technology (rDNA origin) or extracted from animal pancreatic tissue. Multiple FDA-approved formulations exist, including injectable kits, ready-to-use prefilled auto-injectors, and intranasal powder.

Registry IDs

PubChem CID

16132283

CAS

9007-92-5

InChIKey

MASNOZXLGMXCHN-ZLPAWPGGSA-N

Molecular formula

C153H225N43O49S

Molar mass

3482.7 g/mol

Monoisotopic

3480.6157019 Da

InChIKey

MASNOZXLGMXCHN-ZLPAWPGGSA-N

Appearance

Lyophilised white to off-white powder (injectable formulations); off-white intranasal powder (Baqsimi). Reconstituted injectable solution is clear and colourless.

Solubility

Poorly soluble in water at neutral pH; soluble in dilute acid or base. Conventio…

Sequence not available in current seed.

Stability: Glucagon is chemically unstable in neutral aqueous solution, forming amyloid fibrils and losing activity; this was the primary formulation challenge overcome by

Vial sizes

1 mg · 1 mg · null mg

Purity grades

pharmaceutical grade rDNA origin

Salt forms

Free base (primary)

• GHS hazard class on file
• PPE & spill response
• Disposal guidance
• Not-for-human-consumption posture

How much research exists, and of what maturity — never a verdict on whether it works.

Mechanism of action

• Glucagon binds the glucagon receptor (GCGR), a class B G protein-coupled receptor expressed at high density on hepatocytes, activating adenylyl cyclase via Gs coupling to generate cyclic AMP
• Elevated intracellular cAMP activates protein kinase A (PKA), which phosphorylates and activates phosphorylase kinase, ultimately stimulating glycogen phosphorylase and promoting rapid hepatic glycogenolysis to release glucose
• PKA simultaneously phosphorylates and inhibits glycogen synthase, suppressing glycogen formation, while also upregulating gluconeogenic gene expression through the CREB/PGC-1α axis to sustain glucose output during fasting
• In acute hypoglycaemia rescue, glycogenolysis provides the predominant and rapid glycaemic response, with gluconeogenesis becoming increasingly relevant during prolonged fasting as glycogen stores are depleted

Pharmacokinetics (ADME)

Half-life

IV: ~8-18 min; SC: ~42 min apparent (absorption-limited); IM: ~26 min apparent

Clearance

Primarily hepatic and renal proteolytic degradation; moderate plasma clearance ~13.5 mL/min/kg (IV, 1 mg dose). Volume of distribution ~0.25 L/kg.

PK–PD note: SC/IM apparent half-lives are substantially longer than the true elimination half-life due to rate-limited absorption from the injection site. Peak plasma concentrations following SC administration (~…

Reading the evidence

• Evidence quality and gaps vary by application — see the cited grades above.
• Indexed-article counts span all evidence tiers, not only completed human trials.
• No first-party human-dosing, efficacy, or benefit claims are made here.

Key reviews & evidence-gap sources

• Wewer Albrechtsen NJ, et al. 100 years of glucagon and 100 more. Diabetologia. 2023;66(8):1378-1394. PMID: 37367959 — Comprehensive centennial review of glucagon biology and glucagon-based therapies
• Capozzi ME, et al. The past, present, and future physiology and pharmacology of glucagon. Cell Metab. 2022;34(11):1654-1674. PMID: 36323234 — Review covering evolution from impurity to glucagon receptor agonists for T1D
• Kajani S, et al. Hepatic glucagon action: beyond glucose mobilization. Physiol Rev. 2024;104(3):1021-1060. PMID: 38300523 — Physiological Reviews article on hepatic amino acid, ketone body, and mitochondrial actions
• Zeigerer A, et al. Glucagon's Metabolic Action in Health and Disease. Compr Physiol. 2021;11(2):1759-1783. PMID: 33792899 — Pleiotropic metabolic actions of glucagon beyond classical hyperglycemic role
• Rix I, et al. Glucagon Physiology. Endotext [Internet]. MDText.com; updated 2019 — Endotext chapter covering structure, secretion, degradation, and actions of glucagon

5 registered trials — 0 currently recruiting.

NA
NCT02665715
Can Postprandial Reactive Hypoglycaemia be Reduced in Patients After Roux-en-Y Gastric Bypass With a Low Carbohydrate Diet?

COMPLETED

Phase 1
NCT01515579
Comparison of Two Liraglutide Formulations in Healthy Subjects

COMPLETED

Phase 2
NCT00966654
Effect of GLP - 1 (7-36 Amide) on Myocardial Function Following Coronary Artery Bypass (CABG) Surgery

TERMINATED

Phase 4
NCT02616003
Preoperative Condition in Giant Obese Patients

COMPLETED

NA
NCT01460069
The Effect of Glucagon Like Peptide (GLP)-1 in Psoriasis

COMPLETED

Summary (literature)

Per FDA-approved prescribing information for glucagon rDNA origin products: the most common adverse reactions (≥5%) are nausea and vomiting, which are dose-dependent and more frequent at 2 mg doses than at 1 mg. Injection site reactions (oedema, erythema) are occasionally reporte…

WADA status

Not specifically listed as a prohibited substance on the WADA 2026 Prohibited List. Glucagon is an endogenous hormone and an approved therapeutic agent. It does…

Dominant research route: Subcutaneous/Intramuscular (injectable) and Intranasal are the dominant studied and approved routes; IV used as PK reference.

PK in adult volunteers (Cmax 7.9 ng/mL at ~20 min after 1 mg); peak glucose 136 mg/dL at 30 min in 25 volunteers

Bioavailability: Studied following SC administration in adult volunteers; mean peak plasma 7.9 ng/mL at ~20 min post 1 mg dose. No first-pass metabolism (parenteral).

FDA-approved route for severe hypoglycemia (adults and pediatric >20 kg). PK established in adult volunteer studies per FDA label.

PK in adult volunteers (Cmax 6.9 ng/mL at ~13 min after 1 mg); peak glucose 138 mg/dL at 26 min in 25 volunteers; also studied in healthy + IDDM patients (Cmax/AUC identical between groups)

Bioavailability: Mean peak plasma 6.9 ng/mL at ~13 min post 1 mg IM. Apparent t1/2 28.6–31.4 min (longer than IV/IN, attributed to slow release from injection site). Relative bioavailability of intranasal vs IM <30%.

FDA-approved route for severe hypoglycemia. IM served as comparator in intranasal PK studies.

PK in adult volunteers (dose proportionality 0.25–2.0 mg; Vd 0.25 L/kg; clearance 13.5 mL/min/kg; t1/2 8–18 min); also IV infusion studied in 5 healthy + 11 IDDM patients

Bioavailability: 100% bioavailability by definition (parenteral). Dose-proportional PK between 0.25 and 2.0 mg. Elimination t1/2 8–18 min; longer in diabetics (11.9 vs 6.6 min).

FDA-approved route for severe hypoglycemia. Extensively degraded in liver, kidney, and plasma; urinary excretion of intact glucagon not measured.

PK in adults (mean Cmax 6130 pg/mL at ~15 min, 3 mg dose) and pediatric 4–<17 yr (peak 15–20 min; median t1/2 21–31 min); studied in 5 healthy + 11 IDDM patients (1 mg and 2 mg doses); RCT non-inferiority vs IM in T1DM adults

Bioavailability: Relative bioavailability of 1 mg intranasal vs IM <30% (per Pontiroli 1993). Baqsimi (3 mg) achieves mean peak plasma 6130 pg/mL at ~15 min. Common cold/nasal congestion did not impact PK.

FDA-approved as Baqsimi (NDA 210134, approved July 24, 2019) for severe hypoglycemia in adults and pediatric patients ≥4 yr (later ≥1 yr). No inhalation required.

Gastrointestinal stability assessment in human gastric fluid (glucagon metabolized rapidly); no approved oral glucagon product

Bioavailability: Not established as a systemic delivery route. Glucagon (29-aa peptide) is rapidly metabolized in human gastric fluid; oral bioavailability effectively negligible without formulation engineering.

Oral stability only — describes GI degradation, NOT oral absorption. No FDA-approved oral glucagon formulation. Cited stability data from in vitro GI fluid studies.

Animal & human figures are kept visibly separate so studied animal doses are never misread as human guidance.

Sorted A–Z by vendor — never by price

Glucagon is a long-established, off-patent peptide hormone with generic injectable available since 1998; research-grade lab-supplier pricing is stable. Brand formulations (Baqsimi, Gvoke) have seen modest annual increases typical of branded rescue medications. (A cited DrugPatentWatch projection of generic injectable prices at $10–30/vial did not hold up against the same source page on recheck and is dropped rather than repeated as a specific figure.)

Researched storefront prices, bucketed

p25 $87.50 · median $218.00 · p75 $290.00 · 8 researched vendors

Legit, COA-backed band: $50.00–$500.00/mg.

Value rule: don't just buy the cheapest — a price under $3/mg is a red flag. Pair price with COA and independent-test grade.

Estimated cost of research (10 mg)

Vial (best researched price)

$180

Bacteriostatic water (generic estimate)

$6

Syringes / supplies (generic estimate)

$12

What each test proves — general guidance, plus this compound's researched purity data

Purity on the current market (researched)

Synthetic glucagon reference-standard purity determined at 896.36 ± 0.68 mg/g (~89.6%) via mass balance method (Karl Fischer titration, ion chromatography, ICP-MS, and isotope dilution mass spectrometry for peptide impurities), per Wang et al., Scientific Reports 2020. This is a reference-material characterization, not a commercial product purity specification.

Independent labs cited for this compound

One FDA-documented recall found: Eli Lilly Glucagon Emergency Kit lot D239382D (Sept 2021) for loss of potency. No additional glucagon-specific recalls, counterfeit events, or criminal enforcement actions were identified in FDA enforcement reports or WHO medical product alerts as of the search date. WHO falsified-product alerts (Alert N°2/2024) and FDA Import Alert 66-80 pertain to GLP-1 receptor agonists (semaglutide/tirzepatide), not glucagon itself.

Buyer red-flag checklist

• Lyophilized glucagon must remain as powder until reconstitution; a vial found in liquid form indicates degradation and loss of potency (per 2021 Lilly recall).
• Glucagon is inherently unstable as a peptide drug; improper storage or shipping conditions can compromise drug quality and potency.
• Compounded glucagon products are not evaluated by FDA for safety, efficacy, or quality.
• No glucagon-specific FDA import alert exists; Import Alert 66-80 covers GLP-1 receptor agonist bulk drug substances, not glucagon.
• No WHO medical product alerts for falsified glucagon were identified; existing WHO falsified-product alerts target semaglutide (GLP-1), not glucagon.

GMP vs research-grade: the chemistry (SPPS + HPLC + MS) is identical — the difference is the quality system.

Underdosing / mislabeling: No independent lab test data (Janoshik, MZ Biolabs, Finnrick, or equivalent) specific to glucagon peptide products were identified. The 2021 Lilly recall involved a potency-loss defect (liquid instead of lyophilized powder) that functioned as underdosing, but this was a manufacturer-initiated recall, not an independent third-party lab finding.

• An RUO label is not an import exemption — CBP judges actual intended use.
• Lyophilized powder is ambient-stable in transit; temperature control needed for > 7-day transit.
• US-warehouse vendors dodge import scrutiny — they cost more but ship more reliably.

Every item dated & sourced

Not prohibited. Glucagon is not listed on the WADA Prohibited List (not named under S2 peptide hormones/growth factors or S4 hormone and metabolic modulators).

No granted patents identified in current seed. Composition-of-matter coverage is limited given the peptide's synthetic origin.

• IACUC / IRB research context
• RUO buyer responsibilities & documentation
• Veterinary / alternative-use where lawful
• Jurisdiction-aware "who may lawfully obtain"

What people discuss

Reported concerns — discussion, not established effects

Reading caveats

• Diabetes emergency-use context overrepresents negative after-effects
• Retatrutide enthusiasm may inflate positive glucagon-agonism framing
• Mechanism discussion often speculative or inferred from trial data rather than directly measured
• Nasal-format complaints concentrated in Type1Diabetes subreddit may skew format perception

Manually researched from reddit, youtube, x— theme weights are research estimates, not live counts; aggregated & de-identified. No individual posts, quotes, or usernames are ever shown.

Relative research / market volume — populated once the activity stream is wired

Inline tooltips for lyophilized, RUO, EU/mg, SPPS, 503A and more.

Toggle plain-language ↔ scientific in the header.

• How to read a COA
• Free base vs acetate
• Understanding evidence grades

FDA-approved 29-aa pancreatic peptide hormone that raises blood glucose by stimulating hepatic glycogenolysis and gluconeogenesis; used to treat severe hypoglycaemia. Approximately 65,579 articles are indexed (literature last scanned 2026-05-29). US regulatory status: FDA-approved prescription drug (multiple formulations). Research use only.

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