Home Categories Pharmaceutical intermediates Dapagliflozin
A3315012

Dapagliflozin , ≥99% , 461432-26-8

CAS NO.:461432-26-8

Empirical Formula: C21H25ClO6

Molecular Weight: 408.88

MDL number: MFCD13182359

EINECS: 639-683-0

Pack Size Price Stock Quantity
10MG RMB23.20 In Stock
50MG RMB47.20 In Stock
250mg RMB143.20 In Stock
1g RMB389.60 In Stock
5G RMB1119.20 In Stock
25g RMB3648.00 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: 55-58°C
Boiling point: 609.0±55.0 °C(Predicted)
Density  1.349
storage temp.  2-8°C
solubility  DMSO (Slightly), Methanol (Slightly)
pka 13.23±0.70(Predicted)
form  Solid
color  White to Pale Yellow
Stability: Hygroscopic
InChIKey JVHXJTBJCFBINQ-JNTNYNDRNA-N
SMILES O[C@@H]1[C@H]([C@H](O)[C@@H](CO)O[C@H]1C1C=CC(Cl)=C(CC2C=CC(OCC)=CC=2)C=1)O |&1:1,2,3,5,9,r|

Description and Uses

Inhibiting renal glucose reabsorbtion through the sodium-glucose cotransporter (SGLT) offers an insulin-independent alternative to controlling blood glucose concentrations in patients with type 2 diabetes. While the majority of glucose is reabsorbed from glomerular filtrate by SGLT2, which is predominantly expressed in the kidney S1 segment of the proximal tubule, SGLT1 reabsorbs glucose in the distal S3 segment of the renal proximal tubule as well as from the small intestine. Dapagliflozin is a first generation, selective SGLT inhibitor that blocks glucose transport with about 100-fold selectivity for SGLT2 (Ki = 6 nM; EC50 = 1.1 nM) over SGLT1 (Ki = 390 nM). After single oral doses ranging from 0.1 to 1.0 mg/kg, dapagliflozin increases urinary glucose excretion in both normal and diabetic rats, improves glucose tolerance in normal rats, and reduces hyperglycemia in Zucker diabetic fatty rats. Within two weeks of treating diabetic rats with 0.1 to 1.0 mg/kg dapagliflozin, fasting and fed glucose levels have been shown to be significantly lowered as a result of increased glucose utilization accompanied by reduced glucose production.

therapeutic for diabetes I or II, and hyperglycemia

Safety

Symbol(GHS) 
GHS08,GHS07,GHS05
Signal word  Danger
Hazard statements  H302-H372-H318
Precautionary statements  P264-P270-P301+P312-P330-P501-P260-P264-P270-P314-P501-P280-P305+P351+P338-P310

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