카나글리플로진

한글명:카나글리플로진

카스 번호842133-18-0

상품명:Canagliflozin

CBNumberCB02510088

분자식C24H25FO5S

포뮬러 무게444.52

MOL 파일842133-18-0.mol

동의어(한글)

카나글리플로진

화학적 성질

녹는점	68 - 72°C
끓는 점	642.9±55.0 °C(Predicted)
밀도	1.364
저장 조건	-20°C
용해도	DMSO에 용해됨(40mg/ml)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	13.34±0.70(Predicted)
색상	하얀색
안정성	제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO의 솔루션은 -20°C에서 최대 1개월 동안 보관할 수 있습니다.
InChIKey	XTNGUQKDFGDXSJ-XDLHWMRXNA-N
SMILES	O[C@@H]1[C@H]([C@H](O)[C@@H](CO)O[C@H]1C1C=CC(C)=C(CC2=CC=C(C3C=CC(F)=CC=3)S2)C=1)O \|&1:1,2,3,5,9,r\|
CAS 데이터베이스	842133-18-0

위험 및 안전 성명

유해 물질 데이터

842133-18-0(Hazardous Substances Data)

NFPA 704:

	0
3		0

그림문자(GHS)

카나글리플로진 화학적 특성, 용도, 생산

개요
In March 2013, the US FDA approved canagliflozin (JNJ-28431754; TA-7284) for the treatment of type 2 diabetes in adults. Canagliflozin is the first US-approved sodium-glucose co-transporter (SGLT) inhibitor for the treatment of type 2 diabetes. Inhibition of renal SGLT suppresses glucose reabsorption, which permits glucose excretion into urine and reduction of hyperglycemia. Canagliflozin was discovered through structural modifications of phlorizin, a known inhibitor of renal glucose reabsorption. Early modifications of OH groups on the glucose moiety were insufficient to adequately impair hydrolysis by intestinal β-glucosidase. Introduction of the C-glucoside moiety, as in the clinical candidate dapagliflozin, afforded sufficient resistance to hydrolysis. Finally, incorporation of the thiophene moiety in canagliflozin provided improved potency for hSGLT2 (exclusive to kidney), IC₅₀=2.2 nM, while offering significant selectivity over hSGLT1 (in kidney and heart), IC₅₀=910 nM. Hyperglycemic, high-fat (HF) diet fedmice (KKstrain) that received a single 3 mg/kg oral dose of canagliflozin had a 48% reduction in blood glucose levels after 6 h versus vehicle-treatedmice. Noteworthy in themultistep synthesis of canagliflozin is the stereoselective formation of the β-C-glucoside which is accomplished by coupling of the aryllithiumaglycone with 2,3,4,6-tetra-O-trimethylsilyl-β-Dgluconolactone followed by desilylation and stereoselective reduction with triethylsilane and boron trifluoride etherate.
화학적 성질
Pale Yellow Solid
용도
Canagliflozin is a sodium/glucose cotransporter 2 (SGLT2) inhibitor. Canagliflozin has been shown to dose dependently reduce calculated renal threshold for glucose excretion and increase urinary glucose excretion. Canagliflozin is a candidate for the treatment of type 2 diabetes and obesity.
정의
ChEBI: A C-glycosyl compound that is used (in its hemihydrate form) for treatment of type II diabetes via inhibition of sodium-glucose transport protein subtype 2.

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