产品名称

英文名称：PF-04971729

同义词

Ertugliflozin、1210344-57-2、PF-04971729、Steglatro、PF04971729、MK-8835、PF 04971729、(1S,2S,3S,4R,5S)-5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol、UNII-6C282481IP、(1S,2S,3S,4R,5S)-5-[4-chloro-3-[(4-ethoxyphe

产品性质

CAS编号：1210344-57-2

分子式：C22H25ClO7

分子量：436.88

PubChem编号：44814423

英文别名：Ertugliflozin|1210344-57-2|PF-04971729|Steglatro|PF04971729|MK-8835|PF 04971729|(1S,2S,3S,4R,5S)-5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol|UNII-6C282481IP|(1S,2S,3S,4R,5S)-5-[4-chloro-3-[(4-ethoxyphe

规格或纯度：≥98%

英文名称：PF-04971729

生化机理：PF-04971729, a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2, is currently in phase 2 trials for the treatment of diabetes mellitus. Inhibitory effects against the organic cation transporter 2-mediated uptake of [14C]metformin by PF-04971729 also were very weak (IC50 900μM).The disposition of PF-04971729, an orally active selective inhibitor of the sodium-dependent glucose cotransporter 2, was studied after a single 25-mg oral dose of [14C]-PF-04971729 to healthy human subjects. The absorption of PF-04971729 in humans was rapid with a Tmax at ~ 1.0 h. Of the total radioactivity excreted in feces and urine, unchanged PF-04971729 collectively accounted for ~ 35.3% of the dose, sμggestive of moderate metabolic elimination in humans.

储存温度：-20°C储存,充氩

运输条件：超低温冰袋运输

产品介绍：PF-04971729(Ertμgliflozin)是钠离子依赖的葡萄糖协同转运蛋白2（SGLT2）抑制剂。PF-04971729(Ertugliflozin) is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2(SGLT2).Ertugliflozin (MK-8835, PF-04971729) is a potent and selective sodium-dependent glucose cotransporter 2 inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1.

ALogP：1.7

IUPAC Name：(1S,2S,3S,4R,5S)-5-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol

INCHI：InChI=1S/C22H25ClO7/c1-2-28-16-6-3-13(4-7-16)9-14-10-15(5-8-17(14)23)22-20(27)18(25)19(26)21(11-24,30-22)12-29-22/h3-8,10,18-20,24-27H,2,9,11-12H2,1H3/t18-,19-,20+,21-,22-/m0/s1

InChi Key：MCIACXAZCBVDEE-CUUWFGFTSA-N

Canonical SMILES：CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C34C(C(C(C(O3)(CO4)CO)O)O)O)Cl

Isomeric SMILES：CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)[C@@]34[C@@H]([C@H]([C@@H]([C@@](O3)(CO4)CO)O)O)O)Cl

PubChem CID：44814423

ChEMBL Ligand：CHEMBL1770248

CAS Registry No.：1210344-57-2

DrugCentral Ligand：5270

溶解性：Soluble in DMSO

熔点：65 - 66℃

象形图：

信号词：Danger

危险声明：H314 Causes severe skin burns and eye damageH318 Causes serious eye damage

预防措施声明：P280,P321,P405,P501,P264,P260,P301+P330+P331,P304+P340,P363,P264+P265,P305+P354+P338,P317,P302+P361+P354,P316

产品包装