Description
MMV008138 is a species-selective IspD (enzyme 2-C-methyl-d-erythritol 4-phosphate cytidylyltransferase)-targeting antimalarial agent, with an IC50 of 44 nM for PfIspD (P. falciparum IspD). MMV008138 inhibits the growth of P. falciparum Dd2 strain with an IC50 of 250 nM.
Product information
CAS Number: 1679333-73-3
Molecular Weight: 361.22
Formula: C18H14Cl2N2O2
Chemical Name: (1R,3S)-1-(2,4-dichlorophenyl)-1H,2H,3H,4H,9H-pyrido[3,4-b]indole-3-carboxylic acid
Smiles: OC(=O)[C@@H]1CC2=C(NC3C=CC=CC=32)[C@H](N1)C1=CC=C(Cl)C=C1Cl
InChiKey: ZJDRIKAAFJMYGX-JKSUJKDBSA-N
InChi: InChI=1S/C18H14Cl2N2O2/c19-9-5-6-11(13(20)7-9)16-17-12(8-15(22-16)18(23)24)10-3-1-2-4-14(10)21-17/h1-7,15-16,21-22H,8H2,(H,23,24)/t15-,16+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (346.05 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
MMV008138 targets the enzyme IspD in the MEP pathway of P. falciparum. MMV008138 does not target human IspD.
References:
- Ghavami M, et al. Biological Studies and Target Engagement of the 2- C-Methyl-d-Erythritol 4-Phosphate Cytidylyltransferase (IspD)-Targeting Antimalarial Agent (1 R,3 S)-MMV008138 and Analogs. ACS Infect Dis. 2018 Apr 13;4(4):549-559.
- Yao ZK, et al. Determination of the active stereoisomer of the MEP pathway-targeting antimalarial agent MMV008138, and initial structure-activity studies. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1515-9.
Products are for research use only. Not for human use.
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