Ipragliflozin (Synonyms: ASP1941) |
Catalog No.GC16469
One-Click Copy Product Info
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이프라글리플로진(ASP1941)은 인간 SGLT2 및 SGLT1, 쥐 SGLT2 및 SGLT2에 대해 IC50이 각각 7.38 및 1876nM, 6.73 및 1166nM, 5.64 및 1380nM인 경구 활성 및 선택적 SGLT2 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 761423-87-4
Sample solution is provided at 25 µL, 10mM.
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Ipragliflozin is a selective inhibitor of sodium–glucose cotransporter 2 (SGLT2) with IC50 value of 7.38nM [1].
Ipragliflozin is a derivative of phlorizin. It shows inhibition activity for mouse, rat and human SGLT2 with IC50 values of 7.38nM, 6.73nM and 5.64nM, respectively. It is not effective for SGLT1 with IC50 value of 1876nM. In the radioligand binding and enzyme assays, lpragliflozin shows no interaction with other receptors, channels, and transporters like adrenergic, muscarinic and calcium channel, demonstrating a specific inhibition of SGLT2. As a glucitol compound, ipragliflozin is stable against glucosidases in mouse small intestine [1].
Since SGLT2 plays a critical role in renal glucose reabsorption, ipragliflozin is therapeutic potent to treat hyperglycemia in diabetes through increasing glucose excretion into urine. In STZ-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice, the single administration of ipragliflozin significantly decreases the blood glucose levels [1].
References:
[1] Tahara A, Kurosaki E, Yokono M, Yamajuku D, Kihara R, Hayashizaki Y, Takasu T, Imamura M, Qun L, Tomiyama H, Kobayashi Y, Noda A, Sasamata M, Shibasaki M. Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn Schmiedebergs Arch Pharmacol. 2012 Apr;385(4):423-36.
| Cas No. | 761423-87-4 | SDF | |
| Synonyms | ASP1941 | ||
| Chemical Name | (2S,3R,4R,5S,6R)-2-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol | ||
| Canonical SMILES | C1=CC=C2C(=C1)C=C(S2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)F | ||
| Formula | C21H21FO5S | M.Wt | 404.45 |
| Solubility | DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH7.2) (1:7): 0.13 mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4725 mL | 12.3625 mL | 24.7249 mL |
| 5 mM | 494.5 μL | 2.4725 mL | 4.945 mL |
| 10 mM | 247.2 μL | 1.2362 mL | 2.4725 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)