P32/98 hemifumarate

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P32/98 hemifumarate

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

251572-86-8

异亮氨酸噻唑烷半富马酸盐

P32/98 hemifumarate 是一种二肽基肽酶 IV (DPP4) 抑制剂。P32/98 hemifumarate 在 Zucker 糖尿病大鼠模型中可改善葡萄糖耐量、胰岛素敏感性和 β 细胞反应性。

生物活性

P32/98 hemifumarateis a potent inhibitor ofdipeptidyl peptidaseIVwith a K_ivalue of 130 nM. P32/98 hemifumarate improves glucose tolerance,insulinsensitivity and β-cell responsiveness in fatty Zucker rat model^[1]^[2]^[3].

IC₅₀& Target

DPP-4

130 nM (Ki)

体外研究
(In Vitro)

GLP-1 acts function of stimulation of glucose dependent insulin secretion and induction of satiety feelings, and DPPIV is the major renal catabolic pathway for GLP-1 in vivo^[2].
P32/98 hemifumarate, together with 200 pM GLP-1, (10 μM; 3 h) shows no significant inhibition of sodium re-absorption in porcine proximal tubular cells^[2].
P32/98 hemifumarate (10 μM; 96 h) does not influence the mRNA expression of GLP-1R, DPPIV, Na⁺/H⁺exchanger isoform 3 (NHE3), sodium-dependent glucose transporter slc5a1, slc5a2 (SGLT1, 2)^[2].

Cell Cytotoxicity Assay^[2]

Cell Line:	Porcine proximal tubular cells
Concentration:	10 μM
Incubation Time:	96 hours
Result:	Showed no toxic.

体内研究
(In Vivo)

P32/98 hemifumarate (25 mg/kg; i.g.; once daily) long-time treatment significantly improves the glucose tolerance in Zucker diabetic fatty rats, a model of IGT (impaired glucose tolerance)^[3].

Animal Model:	Zucker diabetic fatty rat^[3]
Dosage:	25 mg/kg
Administration:	Oral gavage; once daily
Result:	Significantly improved the glucose tolerance in Zucker diabetic fatty rats.

分子量

260.36

Formula

C₉H₁₈N₂OS.1/2C₄H₄O₄

CAS 号

251572-86-8

中文名称

异亮氨酸噻唑烷半富马酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.