IUB288
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 98.88%
- Formula: C177H272N42O53S
- Molecular Weight:3868.37
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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.
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Cell Line:rat H4IIE hepatoma cells
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Concentration:0.133 nmol/mL
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Incubation Time:120 min
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Result:Significantly increased relative FGF21 mRNA expression in H4IIE cells compared to control.
In Vivo
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.
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Animal Model:C57Bl/6J (male, 11 months old, diet-induced obesity via 9-month high-fat diet)[1]
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Dosage:0.3 nmol/kg/day; 1 nmol/kg/day; 3 nmol/kg/day; 10 nmol/kg/day
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Administration:daily; up to 18 days
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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.
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Animal Model:db/db (male, 12 weeks old, leptin receptor-deficient, type 2 diabetes)[1]
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Dosage:10 nmol/kg/day
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Administration:daily; 7 days
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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.
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Animal Model:C57Bl/6J (male, 12 weeks old, wild-type and FGF21-deficient littermates, obesity prevention via high-fat diet initiation)[1]
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Dosage:10 nmol/kg/day
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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.
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Animal Model:C57Bl/6J (male, 11 months old, diet-induced obesity via 9-month high-fat diet)[1]
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Dosage:10 nmol/kg/day
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Administration:daily; 18 days
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Result:Increased hepatic FGF21 mRNA expression to ~7-fold relative to vehicle.
Increased plasma FGF21 to ~400 pg/dL.
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Animal Model:C57Bl/6J (diet-induced obese, high-fat diet fed)[2]
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Dosage:10 nmol/kg
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Administration:s.c.; daily
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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.
Chemical Information
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Appearance Solid
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Molecular Weight 3868.37
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Formula C177H272N42O53S
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Color White to off-white
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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
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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
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Sequence Shortening
H-Aib-QGTFISD-Lys(γGlu-γGlu-C16)-SKYLD-Aib-RAAQDFVQWLMDT
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 33.33 mg/mL (8.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.67 mg/mL (0.43 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (293 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.2585 mL | 1.2925 mL | 2.5851 mL | 6.4627 mL |
| 5 mM | 0.0517 mL | 0.2585 mL | 0.5170 mL | 1.2925 mL |
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