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AR 231453

产品编号: DC8764 Featured
AR 231453
结构式
733750-99-7
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中国地区超过5000个高品质化合物库存
应用领域
AR 231453是一种有效，选择性和可口服的 GPR119 激动剂。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 733750-99-7
名称:
别名: AR231453; AR-231453
SMILES: FC1C=C(S(C)(=O)=O)C=CC=1NC1C([N+]([O-])=O)=C(N2CCC(C3ON=C(C(C)C)N=3)CC2)N=CN=1
分子式: C21H24FN7O5S
分子量: 505.52
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: AR231453 is a potent and selective small molecule agonist of GPR119 that enhances glucose-dependent insulin secretion and glucagon-like peptide 1 (GLP-1) release; Antidiabetic agent.in vitro: The GPR119-specific agonist AR231453 significantly increased cAMP accumulation and insulin release in both HIT-T15 cells and rodent islets. In both cases, loss of GPR119 rendered AR231453 inactive. In GLUTag cells, a well-established model of intestinal L-cell function, the potent GPR119 agonist AR231453 stimulated cAMP accumulation and GLP-1 release. in vivo: AR231453 also enhanced glucose-dependent insulin release in vivo and improved oral glucose tolerance in wild-type mice but not in GPR119-deficient mice. Diabetic KK/A(y) mice were also highly responsive to AR231453. Orally active GPR119 agonists may offer significant promise as novel antihyperglycemic agents acting in a glucose-dependent fashion. When administered in mice, AR231453 increased active GLP-1 levels within 2 min after oral glucose delivery and substantially enhanced total glucose-dependent insulinotropic peptide levels. Blockade of GLP-1 receptor signaling with exendin(9-39) reduced the ability of AR231453 to improve glucose tolerance in mice.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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