A 922500（DGAT-1抑制剂4a）是一种强效、选择性和口服生物利用度的甘油二酰基转移酶1（DGAT-1）抑制剂，其对人类和小鼠DGAT-1的IC50值分别为9 nM和22 nM。
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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
A-922500 exhibits high selectivity against other acyltransferases, such as DGAT-2, with an IC50 value of 53 μM, and is also selective over its phylogenetic relatives, acyl coenzyme A cholesterol acyltransferase-1 and -2, with an IC50 value of 296 μM[1].
A 922500 动物研究
Animal study
A 922500 has been shown to decrease serum triglyceride levels across all tested dosages. Notably, a dosage of 3 mg/kg significantly reduced serum triglycerides by 53%. This same dosage also led to a 55% reduction in serum free fatty acid (FFA) concentrations and a 25% decrease in total cholesterol. However, DGAT-1 inhibition did not significantly impact body weight at any tested dosage. While A 922500 did not significantly alter LDL-cholesterol or HDL-cholesterol levels individually, it did significantly improve the serum LDL/HDL-cholesterol ratio at dosages of 0.3 and 3 mg/kg[1].
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