Sitagliptin phosphate

한글명:Sitagliptin phosphate

카스 번호654671-78-0

상품명:Sitagliptin phosphate

CBNumberCB71179744

분자식C16H15F6N5O.H3PO4

포뮬러 무게505.31

MOL 파일654671-78-0.mol

화학적 성질

녹는점	202-204°C
저장 조건	-20°C Freezer
용해도	메탄올(약간 용해됨, 가열), 물(소량으로 용해, 초음파 처리)
물리적 상태	고체
물리적 상태	단단한 모양
색상	흰색에서 황백색까지
InChI	InChI=1S/C16H15F6N5O.H3O4P/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22;1-5(2,3)4/h4,6,9H,1-3,5,7,23H2;(H3,1,2,3,4)
InChIKey	IQFYVLUXQXSJJN-UHFFFAOYSA-N
SMILES	C(C1=CC(F)=C(F)C=C1F)C(N)CC(=O)N1CCN2C(C(F)(F)F)=NN=C2C1.P(O)(O)(O)=O

그림문자(GHS)

Sitagliptin phosphate 화학적 특성, 용도, 생산

개요
Sitagliptin is the first novel dipeptidyl peptidase IV inhibitor from Merck for the treatment of type 2 diabetes without weight gain and the incidence of hypoglycemia was similar to placebo. Sitagliptin acts by enhancing the body’s incretin system, which helps to regulate glucose by affecting β and α cells in the pancreas.
화학적 성질
White Solid
용도
A trizolopyrazine dipeptidyl peptidase IV inhibitor. It has recently been approved for the therapy of type II diabetes.
일반 설명
Sitagliptin phosphate is the 1:1 phosphoric acid salt ofsitagliptin free base (i.e., (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)-2-butanamine), and is marketed(Junuvia, 2006) in 25-, 50-, and 100-mg tablets. Acombination product with metformin (Janumet, 2007) intwo strengths (50 mg/500 mg and 50 mg/1,000 mgsitagliptin/metformin) is also available, and sitagliptin mayalso be prescribed with a thiazolidinedione, or possibly a sulfonylurea.The phosphate salt provides very high water solubility.The bioavailability of orally administered sitagliptinis～87%. The drug exhibits relatively low plasma protein binding (～38%), a relatively large volume of distribution(198 L), and a terminal elimination half-life of 12 hours.About 79% of a 100-mg oral dose is excreted unchanged inurine, the balance as trace-level metabolites (CYP3A4, lessercontribution by CYP2C8) in urine or feces: 87% of administeredradioactivity is excreted in urine, and 13% in feces.Active tubular excretion is reported to play a key role in renalclearance of unchanged drug, and may be mediated at least inpart via the organic anion transporter hOAT-3.

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