EGT1442 - CAS 1118567-05-7
Catalog number:
1118567-05-7
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C24H29ClO7
Molecular Weight:
464.94
COA:
Inquire
Targets:
SGLT
Description:
EGT1442 is a potent and selective SGLT2 inhibitor with IC50 value of 5.6 μM /2 nM in SGLT1 /SGLT2 respectively. It significantly prolonged the median survival of SHRSP rats. It attenuates blood glucose and HbA(1c) levels and prolongs the survival of stroke-prone rats in db/db mice. It showed favorable properties both in vitro and in vivo and could be beneficial to the management of type 2 diabetic patients. It was developed by Theracos and in clinic phase 1 trials.
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Purity:
>98%
Appearance:
Solid powder
Synonyms:
(1S)-1,5-Anhydro-1-C-[4-chloro-3-[[4-[2-(cyclopropyloxy)ethoxy]phenyl]methyl]phenyl]-D-glucitol;Bexagliflozin;THR1442;EGT0001442;EGT-1442;THR-1442;EGT-0001442;(2S,4R,6R)-2-(4-chloro-3-(4-(2-cyclopropoxyethoxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol;(3R,4R,5S,6R)-2-(4-chloro-3-(4-(2-cyclopropoxyethoxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol
Solubility:
Soluble to 35mg/mL in CD3OD
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
EGT1442 showed favorable properties and could be beneficial to the management of type 2 diabetic patients.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
671.0±55.0 °C | Condition: Press: 760 Torr
Density:
1.41±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
BTCRKOKVYTVOLU-HCGOJEOKSA-N
InChI:
InChI=1S/C24H29ClO7/c25-19-8-3-15(24-23(29)22(28)21(27)20(13-26)32-24)12-16(19)11-14-1-4-17(5-2-14)30-9-10-31-18-6-7-18/h1-5,8,12,18,20-24,26-29H,6-7,9-11,13H2/t20-,21?,22+,23?,24+/m1/s1
Canonical SMILES:
C1CC1OCCOC2=CC=C(C=C2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)Cl
Current Developer:
EGT1442 was developed by Theracos and in clinic phase 1 trials.
1.EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats.
Zhang W1, Welihinda A, Mechanic J, Ding H, Zhu L, Lu Y, Deng Z, Sheng Z, Lv B, Chen Y, Roberge JY, Seed B, Wang YX. Pharmacol Res. 2011 Apr;63(4):284-93. doi: 10.1016/j.phrs.2011.01.001. Epub 2011 Jan 5.
Sodium glucose co-transporter 2 (SGLT2) is a renal type III integral membrane protein that co-transports sodium and glucose from filtrate to epithelium in the proximal tubule. Human subjects with homozygous or compound heterozygous mutations in SLC5A2 exhibit glucosuria without hypoglycemia or other obvious morbidity, suggesting that blockade of SGLT2 has the potential to promote normalization of blood glucose without hypoglycemia in the setting of type 2 diabetes. This report presents the in vitro and in vivo pharmacological activities of EGT1442, a recently discovered SGLT2 inhibitor in the C-aryl glucoside class. The inhibitory effects of EGT1442 for human SGLT1 and SGLT2 were evaluated in an AMG uptake assay and the in vivo efficacy of treatment with EGT1442 was investigated in rats and dogs after a single dose and in db/db mice after chronic administration. The effect of EGT1442 on median survival of SHRSP rats was also evaluated. The IC(50) values for EGT1442 against human SGLT1 and SGLT2 are 5.
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CAS 1118567-05-7 EGT1442

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