KBP-089
Based on 1 Customer Validation
KBP-089 is a dual Amylin and Calcitonin Receptor agonist. KBP-089 reduces body weight, decreases adipose tissue mass and improves glucose tolerance in obese rats. KBP-089 also eliminates lipid accumulation in the liver and muscle, and ameliorates glycemic homeostasis and insulin sensitivity. KBP-089 is applicable to the research of diseases such as obesity and type 2 diabetes.
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- Pureté: 99.42%
- CAS No.: 1776112-67-4
- Formule: C148H242N46O48S3
- Masse moléculaire:3529.98
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Stockage:
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
KBP-089 (3 h) potently activates human CTR and AMY3-R in heterologous cell lines with its pEC50 values ranging from 8.7 to 9.9, and can induce sustained receptor activation for up to 72 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
KBP-089 (0.625-40 μg/kg; s.c.; 6 weeks) reduces body weight and improves glucose tolerance in high-fat diet-fed rats following 4-fold dose escalation administration[1].
KBP-089 (0.625-40 μg/kg; s.c.; single dose) dose-dependently suppresses caloric intake in overnight-fasted high-fat diet-fed rats within 48 h[1].
KBP-089 (5-20 μg/kg; s.c.; 8 weeks total) reduces blood glucose levels, improves glucose tolerance and enhances insulin action in diabetic obese rats[2].
KBP-089 (2.5 µg/kg; s.c.; 7 days) reduces total caloric intake in rats fed a normal diet and shifts their food preference from chocolate to standard chow[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley (male, 18 weeks of age, high-fat diet-induced obesity model)[1]
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Dosage:0.625, 2.5, 10, 40 μg/kg
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Administration:s.c.; 4-fold dose escalation followed by 6 weeks of maintenance at final dose
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Result:Induced transient food intake reduction at each dose escalation step (magnitude decreasing over time).
Caused ~15% vehicle-corrected weight loss, corresponding adipose tissue reduction, and improved oral glucose tolerance at 2.5, 10, or 40 μg/kg.
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Animal Model:Zucker Diabetic Fatty (ZDF-Leprfa/Crl) rats (male, 6 weeks old)[2]
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Dosage:5 µg/kg (first 4 weeks) and 20 µg/kg (additional 4 weeks)
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Administration:s.c.; daily; 8 weeks total
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Result:Reduced fasting blood glucose over 7 weeks.
Reduced HbA1c at study end; Lowered oral glucose tolerance test tAUC.
Increased insulin sensitivity.
Chemical Information
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CAS No. 1776112-67-4
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Appearance Solid
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Masse moléculaire 3529.98
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Formule C148H242N46O48S3
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Color White to off-white
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Sequence
Ac-Cys-Ser-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Arg-Leu-Ser-Gln-Asp-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Lys-Thr-Asp-Val-Gly-Ala-Asn-Ala-Pro-NH2 (Disulfide bridge: Cys1-Cys7)
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Sequence Shortening
Ac-CSNLSTCMLGRLSQDLHRLQTYPKTDVGANAP-NH2 (Disulfide bridge: Cys1-Cys7)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (28.33 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: ≥ 2.5 mg/mL (0.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (0.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureté et documentation
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Fiche technique (290 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Gydesen S, et al. Optimization of tolerability and efficacy of the novel dual amylin and calcitonin receptor agonist KBP-089 through dose escalation and combination with a GLP-1 analog. Am J Physiol Endocrinol Metab. 2017 Nov 1;313(5):E598-E607. [Content Brief]
[2]. Gydesen S, et al. A novel dual amylin and calcitonin receptor agonist, KBP-089, induces weight loss through a reduction in fat, but not lean mass, while improving food preference. Br J Pharmacol. 2017 Apr;174(7):591-602. [Content Brief]
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 | 0.2833 mL | 1.4164 mL | 2.8329 mL | 7.0822 mL |
| 5 mM | 0.0567 mL | 0.2833 mL | 0.5666 mL | 1.4164 mL | |
| 10 mM | 0.0283 mL | 0.1416 mL | 0.2833 mL | 0.7082 mL | |
| 15 mM | 0.0189 mL | 0.0944 mL | 0.1889 mL | 0.4721 mL | |
| 20 mM | 0.0142 mL | 0.0708 mL | 0.1416 mL | 0.3541 mL | |
| 25 mM | 0.0113 mL | 0.0567 mL | 0.1133 mL | 0.2833 mL |
KBP-089 Related Classifications
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