CID 2745687 (Synonyms: ML-194) |
| Katalog-Nr.GC10483 |
CID 2745687 wirkt als spezifischer, reversibler und kompetitiver GPR35-Antagonist mit einem Ki von 12,8 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 264233-05-8
Sample solution is provided at 25 µL, 10mM.
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pIC50: 6.70 for human GPR35
CID-2745687 is a GPR35 antagonist. GPR35 is a poorly characterized member of the rhodopsinlike, class A subfamily of G protein-coupled receptors (GPCRs). GPCRs, based on the expression pattern, has been considered as a possible therapeutic target in conditions including diabetes, cardiovascular disease, as well as inflammation and pain.
In vitro: Previous study indicated that both CID-2745687 and ML-145 could competitively inhibit the effects of cromolyn disodium and zaprinast (two agonists sharing an overlapping binding site) on human GPR35. In contrast, though ML-145 antagonized the effects of pamoate competitively, CID-2745687 showed a noncompetitive fashion. Additionally, neither ML-145 nor CID-2745687 was able to antagonize the agonist effects at rodent ortholog of GPR35 [1].
In vivo: To test whether GPR35 contributes to the metabolic effect of Zaprinast, the retina from Cngb1/ mice was preincubated with a GPR35 antagonist, CID-2745687, followed by an additional Zaprinast treatment. Results showed that CID-2745687 did not block the effect of Zaprinast on glutamate and aspartate. Moreover, pamoic acid, the GPR35 agonist, did not change aspartate or glutamate levels [1].
Clinical trial: N/A
References:
[1] Jenkins L,Harries N,Lappin JE,MacKenzie AE,Neetoo-Isseljee Z,Southern C,McIver EG,Nicklin SA,Taylor DL,Milligan G. Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. J Pharmacol Exp Ther.2012 Dec;343(3):683-95.
[2] Du J,Cleghorn WM,Contreras L,Lindsay K,Rountree AM,Chertov AO,Turner SJ,Sahaboglu A,Linton J,Sadilek M,Satrústegui J,Sweet IR,Paquet-Durand F,Hurley JB. Inhibition of mitochondrial pyruvate transport by zaprinast causes massive accumulation of aspartate at the expense of glutamate in the retina. J Biol Chem.2013 Dec 13;288(50):36129-40.
| Cas No. | 264233-05-8 | SDF | |
| Überlieferungen | ML-194 | ||
| Chemical Name | (E)-methyl 5-((2-(tert-butylcarbamothioyl)hydrazono)methyl)-1-(2,4-difluorophenyl)-1H-pyrazole-4-carboxylate | ||
| Canonical SMILES | S=C(N/N=C/C1=C(C(OC)=O)C=NN1C(C(F)=C2)=CC=C2F)NC(C)(C)C | ||
| Formula | C17H19F2N5O2S | M.Wt | 395.43 |
| Löslichkeit | DMSO: 10 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 | 2.5289 mL | 12.6445 mL | 25.2889 mL |
| 5 mM | 0.5058 mL | 2.5289 mL | 5.0578 mL |
| 10 mM | 0.2529 mL | 1.2644 mL | 2.5289 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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.
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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