KBP-066A
KBP-066A is a long-acting dual amylin and calcitonin receptor agonist. KBP-066A can activate the CTR and AMY-R potently, with no off-target activity. KBP-066A reduces fasting blood glucose levels, fasting insulin levels, and body weight in diabetic rat models. KBP-066A can be used for the research of type 2 diabetes mellitus, obesity.
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- Fòrmula: C182H303N47O60S2
- Peso molecular:4173.76
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
In Vitro
KBP-066A (0-25 μM) binds to AMY3R in a concentration-dependent manner[1].
KBP-066A activates CTR (U20S CALCR) and AMY3R (CHO K1 CALCR RAMP3) cells with no off-target activity on tested calcitonin-like receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
KBP-066A (0.75-3 nmol/kg; s.c.; every third day; 8 weeks) improves glycemic status in diabetic ZDF rats[1].
KBP-066A (0.5-36 nmol/kg; s.c.; single dose) has a dose-dependent acute effect on reducing food intake and body weight in obese rats, with longer duration at higher doses[1].
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, 5-6 weeks old at arrival, baseline weight 528.2 ± 27.9 g at study start, obese via 60 kcal% fat high-fat diet for 20 weeks)[1]
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Dosage:1, 2, 4 nmol/kg
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Administration:s.c.; every third day; 4 weeks
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Result:Reduced body weight tAUC to 2584 ± 7, 2452 ± 6, 2458 ± 8 g days⁻¹ vs. vehicle 2773 ± 4 g days⁻¹.
Reduced accumulated food intake tAUC to 617 ± 10, 518 ± 6, 532 ± 10 g days⁻¹ vs. vehicle 811 ± 11 g days⁻¹.
Reduced perirenal adipose tissue in 2 and 4 nmol/kg groups.
Improved oral glucose tolerance (non-significant iAUC vs. vehicle).
Reduced plasma insulin iAUC and HOMA-IR significantly.
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Animal Model:Zucker Diabetic Fatty (ZDF) (male, 5-6 weeks old at arrival, baseline weight 334.1 ± 15.5 g, baseline fasting blood glucose 14 ± 5.1 mM, baseline plasma insulin 8.0 ± 3.9 ng/mL)[1]
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Dosage:0.75, 1.5, 3 nmol/kg
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Administration:S.c.; every third day; 8 weeks
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Result:Reduced fasting blood glucose tAUC to 6180 ± 67, 6405 ± 89, 6409 ± 122 vs. vehicle 6475 ± 103.
Reduced accumulated food intake tAUC to 3815 ± 135, 3134 ± 111, 2898 ± 61 g*days⁻¹ vs. vehicle 4453 ± 123 g*days⁻¹.
Reduced HbA1c and significantly improved oral glucose tolerance iAUC at 3 nmol/kg dose.
Showed no significant body weight reduction.
Chemical Information
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Peso molecular 4173.76
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Fòrmula C182H303N47O60S2
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Sequence
Ac-Cys-Ser-Asn-Leu-Ser-Thr-Cys-{Aib}-Leu-Gly-{Lys(2OEG-γGlu-C18 diacid)}-Leu-Ser-Gln-Asp-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Lys-Thr-Asp-Val-Gly-Ala-Asn-Ala-Pro-NH2
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Sequence Shortening
Ac-CSNLSTC-{Aib}-LG-{K(2OEG-γGlu-C18 diacid)}-LSQDLHRLQTYPKTDVGANAP-NH2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KBP-066A Related Classifications
HY-P11584 Related Classifications
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