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CVT-12012

رقم الكتالوجGC31447

CVT-12012 هو مثبط قوي ومتوفر حيوياً لـ stearoyl-coA desaturase (SCD) ، مع IC50s من 38 نانومتر ، 6.1 نانومتر للجرذان الميكروسومي والإنسان HEPG2 ، على التوالي

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CVT-12012 التركيب الكيميائي

Cas No.: 1018675-35-8

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
99٫00
متوفر
1mg
36٫00
متوفر
5mg
90٫00
متوفر
10mg
135٫00
متوفر
25mg
243٫00
متوفر
50mg
365٫00
متوفر
100mg
540٫00
متوفر

Tel:(909) 407-4943 Email: sales@glpbio.com


مراجعات العميل

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  • GlpBio Citations

    GlpBio Citations
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Sample solution is provided at 25 µL, 10mM.

Description of CVT-12012

CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.

CVT-12012 (Compound 5b) displays the highest potency in both the microsomal and the HEPG2 SCD assays (IC50 38 nM and 6.1 nM, respectively) compared to the other methyl-substituted compounds[1].

In a rat PK study, CVT-12012 demonstrates good oral bioavailability (78%). It appears that the oral absorption of CVT-12012 is not affected by a significant Pgp efflux, which is expected based on Caco-2 assay result. The plasma clearance of CVT-12012 is high (88 mL/min/kg) with elimination half-life of approximately 1 h[1].

[1]. Koltun DO, et al. Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4070-4. [2]. Atkinson KA, et al. N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1621-5.

Chemical Properties of CVT-12012

Cas No. 1018675-35-8 SDF
Canonical SMILES O=C(NCCN1C(C(C)=NC2=C1C=C(NCC3=CC=CC(C(F)(F)F)=C3)C=C2)=O)CO
Formula C21H21F3N4O3 M.Wt 434.41
الذوبان DMSO : 125 mg/mL (287.75 mM) 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of CVT-12012

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.302 mL 11.5099 mL 23.0197 mL
5 mM 0.4604 mL 2.302 mL 4.6039 mL
10 mM 0.2302 mL 1.151 mL 2.302 mL
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In vivo Formulation Calculator (Clear solution) of CVT-12012

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.)

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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 ddH2O, 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.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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