KBP-089
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1776112-67-4
- 分子式: C148H242N46O48S3
- 分子量:3529.98
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
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.
化学情報
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CAS 番号 1776112-67-4
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分子量 3529.98
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分子式 C148H242N46O48S3
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配列
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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シーケンスの短縮
Ac-CSNLSTCMLGRLSQDLHRLQTYPKTDVGANAP-NH2 (Disulfide bridge: Cys1-Cys7)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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