2. GPCR/G Protein Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. GCGR GLP Receptor FGFR HMG-CoA Reductase (HMGCR)
  4. IUB288

IUB288 is a stable and long-acting glucagon-modified peptide, as well as a highly selective Glucagon Receptor agonist. IUB288 stimulates the production of cAMP, increases the expression levels of FGF21 in plasma and liver, regulates bile acid metabolism, and inhibits the expression of hepatic HMGCR. IUB288 improves hypercholesterolemia, enhances insulin sensitivity, increases core body temperature, boosts energy expenditure, suppresses food intake, and can also induce hyperglycemia and glucose intolerance. IUB288 is applicable to the research of diet-induced obesity, type 2 diabetes, and obesity-related glucose intolerance.

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IUB288

IUB288 Chemical Structure

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IUB288 Related Antibodies

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Description

IUB288 is a stable and long-acting glucagon-modified peptide, as well as a highly selective Glucagon Receptor agonist. IUB288 stimulates the production of cAMP, increases the expression levels of FGF21 in plasma and liver, regulates bile acid metabolism, and inhibits the expression of hepatic HMGCR. IUB288 improves hypercholesterolemia, enhances insulin sensitivity, increases core body temperature, boosts energy expenditure, suppresses food intake, and can also induce hyperglycemia and glucose intolerance. IUB288 is applicable to the research of diet-induced obesity, type 2 diabetes, and obesity-related glucose intolerance[1][2].

IC50 & Target[1]

FGF21

 

GLP-1

 

In Vitro

IUB288 (0.0001-10 nM; 5 h) potently activates the glucagon receptor in HEK293 cells with enhanced activity relative to native glucagon[1].
IUB288 (0.0001-10 nM; 5 h) activates the GLP-1 receptor in HEK293 cells with approximately 100-fold lower potency than at the glucagon receptor, demonstrating high GcgR selectivity[1].
IUB288 (0.133 nmol/mL; 120 min) significantly upregulates FGF21 gene expression in rat H4IIE hepatoma cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

IUB288 Related Antibodies

Real Time qPCR[1]

Cell Line: rat H4IIE hepatoma cells
Concentration: 0.133 nmol/mL
Incubation Time: 120 min
Result: Significantly increased relative FGF21 mRNA expression in H4IIE cells compared to control.
In Vivo

IUB288 (0.3-10 nmol/kg/day; daily; up to 18 days) produces potent body weight and fat mass loss, reduces plasma cholesterol, increases blood glucose, and suppresses hepatic HMGCR expression in diet-induced obese male C57Bl/6J mice[1].
IUB288 (10 nmol/kg; i.p.; single dose) increases blood glucose in chow-fed mice and stimulates transient FGF21 secretion in obese mice, while IUB288 (10 nmol/kg/day; daily; 16 days) chronic treatment increases food intake and plasma triglycerides without altering body weight in chow-fed mice[1].
IUB288 (10 nmol/kg/day; daily; 7 days) reduces body weight, increases core body temperature, and enhances insulin sensitivity in leptin receptor-deficient db/db mice without altering blood glucose or food intake[1].
IUB288 (10 nmol/kg/day; daily; 20 days) prevents diet-induced weight gain, increases EE, and reduces plasma cholesterol in WT mice, but these effects are ablated in FGF21-deficient mice, demonstrating FGF21 is required for most long-term metabolic actions of IUB288[1].
IUB288 (10 nmol/kg/day; daily; 18 days) increases hepatic FGF21 expression and circulating FGF21 levels in diet-induced obese mice[1].
IUB288 (10 nmol/kg; s.c.; daily) reduces body weight and suppresses food intake in diet-induced obese C57Bl/6J mice, and its associated glucose intolerance is rescued by co-treatment with bile acid sequestration resins, which also enhance its anti-obesity effect[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57Bl/6J (male, 11 months old, diet-induced obesity via 9-month high-fat diet)[1]
Dosage: 0.3 nmol/kg/day; 1 nmol/kg/day; 3 nmol/kg/day; 10 nmol/kg/day
Administration: daily; up to 18 days
Result: Lowered initial body weight by nearly 30% at 10 nmol/kg/day.
Decreased cumulative food intake at 10 nmol/kg/day.
Elevated ad libitum blood glucose in a dose-dependent manner.
Diminished fat mass at 10 nmol/kg/day
Corrected hypercholesterolemia, lowering plasma cholesterol from approximately 125 mg/dL to 65 mg/dL at 10 nmol/kg/day.
Inhibited hepatic 3-hydroxy-3-methylglutaryl coenzyme-A reductase (HMGCR) expression at 10 nmol/kg/day
Raised plasma triglycerides in chow-fed mice at 10 nmol/kg/day.
Exerted no obvious body weight reduction at doses of 0.3, 1, and 3 nmol/kg/day.
Animal Model: db/db (male, 12 weeks old, leptin receptor-deficient, type 2 diabetes)[1]
Dosage: 10 nmol/kg/day
Administration: daily; 7 days
Result: Decreased relative body weight to around 95% of baseline weight on day 7.
Elevated core body temperature.
Produced no changes in ad libitum and fasting blood glucose.
Strengthened insulin sensitivity and accelerated glucose disappearance rate (Kd).
Exerted no obvious shifts in food intake compared with vehicle group.
Animal Model: C57Bl/6J (male, 12 weeks old, wild-type and FGF21-deficient littermates, obesity prevention via high-fat diet initiation)[1]
Dosage: 10 nmol/kg/day
Administration: unspecified route, daily; 20 days
s.c., daily; 72 hours
Result: Lowered body weight to approximately 88% of starting weight in WT mice.
Diminished fat mass in WT mice.
Decreased lean mass in WT mice.
Elevated cumulative energy expenditure (EE) in WT mice.
Boosted locomotor activity during light phase in WT mice.
Lowered plasma cholesterol levels in WT mice.
Raised ad libitum blood glucose concentrations in WT mice.
Exerted no detectable impacts on body weight, fat mass, lean mass, EE or locomotor activity in FGF21-/- mice.
Lost the capacity to lower plasma cholesterol in FGF21-/- mice.
Triggered stronger elevations of plasma triglycerides and nonesterified free fatty acids (NEFAs) in FGF21-/- mice compared with WT mice.
Caused milder elevation of ad libitum blood glucose in FGF21-/- mice relative to WT mice.
Provoked glucose intolerance in both WT and FGF21-/- mice against corresponding vehicle groups.
Animal Model: C57Bl/6J (male, 11 months old, diet-induced obesity via 9-month high-fat diet)[1]
Dosage: 10 nmol/kg/day
Administration: daily; 18 days
Result: Increased hepatic FGF21 mRNA expression to ~7-fold relative to vehicle.
Increased plasma FGF21 to ~400 pg/dL.
Animal Model: C57Bl/6J (diet-induced obese, high-fat diet fed)[2]
Dosage: 10 nmol/kg
Administration: s.c.; daily
Result: Reduced body weight in diet-induced obese mice.
Suppressed food intake in diet-induced obese mice.
Caused glucose intolerance in diet-induced obese mice.
Restored glucose excursion to the levels of vehicle-treated controls when co-administered with 3% Cholestyramine supplemented high-fat diet.
Enhanced weight loss when co-administered with 3% or 1.5% Cholestyramine, or 2% or 4% Colesevelam supplemented high-fat diet.
Completely suppressed food intake when co-administered with 4% Colesevelam supplemented high-fat diet.
Reduced yet failed to fully suppress food intake when co-administered with 2% Colesevelam supplemented high-fat diet.
Molecular Weight

3868.37

Formula

C177H272N42O53S
Sequence

His-Aib-Gln-Gly-Thr-Phe-Ile-Ser-Asp-Lys-Ser-Lys(γGlu-γGlu-C16)-Tyr-Leu-Asp-Aib-Arg-Ala-Ala-Gln-Asp-Phe-Val-Gln-Trp-Leu-Met-Asp-Thr
Sequence Shortening

H-Aib-QGTFISD-Lys(γGlu-γGlu-C16)-SKYLD-Aib-RAAQDFVQWLMDT
SMILES

O=C(NC(C)(C)C(N[C@@H](CCC(N)=O)C(NCC(N[C@@H]([C@H](O)C)C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CO)C(N[C@@H](CC(O)=O)C(N[C@@H](CCCCNC(CC[C@H](NC(CC[C@H](NC(CCCCCCCCCCCCCCC)=O)C(O)=O)=O)C(O)=O)=O)C(N[C@@H](CO)C(N[C@@H](CCCCN)C(N[C@@H](CC2=CC=C(C=C2)O)C(N[C@@H](CC(C)C)C(N[C@@H](CC(O)=O)C(NC(C)(C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C)C(N[C@@H](C)C(N[C@@H](CCC(N)=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CC3=CC=CC=C3)C(N[C@@H](C(C)C)C(N[C@@H](CCC(N)=O)C(N[C@@H](CC4=CNC5=CC=CC=C45)C(N[C@@H](CC(C)C)C(N[C@@H](CCSC)C(N[C@@H](CC(O)=O)C(N[C@@H]([C@H](O)C)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC6=CNC=N6)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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IUB288 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IUB288IUB 288IUB-288GCGRGLP ReceptorFGFRHMG-CoA Reductase (HMGCR)Glucagon ReceptorFibroblast growth factor receptorleptin receptor-deficient db/db micetype 2 diabetesFGF21-deficient micebile acid metabolismHEK293 cellsdiet-induced obese male C57Bl/6J miceFGF21glucagon receptorrat H4IIE hepatoma cellsHMGCRInhibitorinhibitorinhibit

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