Product Name :
MLT-943
Description:
MLT-943 is a potent, selective and orally active MALT1 protease inhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MLT-943 has anti-inflammatory activities and can be used for FcgR-mediated inflammation research.
CAS:
1832576-04-1
Molecular Weight:
414.77
Formula:
C16H14ClF3N6O2
Chemical Name:
3-{2-chloro-7-[(1S)-1-methoxyethyl]pyrazolo[1,5-a]pyrimidin-6-yl}-1-[2-(trifluoromethyl)pyridin-4-yl]urea
Smiles :
CO[C@@H](C)C1=C(C=NC2=CC(Cl)=NN21)NC(=O)NC1=CC(=NC=C1)C(F)(F)F
InChiKey:
ZMPUACZRXUZAJD-QMMMGPOBSA-N
InChi :
InChI=1S/C16H14ClF3N6O2/c1-8(28-2)14-10(7-22-13-6-12(17)25-26(13)14)24-15(27)23-9-3-4-21-11(5-9)16(18,19)20/h3-8H,1-2H3,(H2,21,23,24,27)/t8-/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
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.
Additional information:
MLT-943 is a potent, selective and orally active MALT1 protease inhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MLT-943 has anti-inflammatory activities and can be used for FcgR-mediated inflammation research.|Product information|CAS Number: 1832576-04-1|Molecular Weight: 414.77|Formula: C16H14ClF3N6O2|Chemical Name: 3-{2-chloro-7-[(1S)-1-methoxyethyl]pyrazolo[1,5-a]pyrimidin-6-yl}-1-[2-(trifluoromethyl)pyridin-4-yl]urea|Smiles: CO[C@@H](C)C1=C(C=NC2=CC(Cl)=NN21)NC(=O)NC1=CC(=NC=C1)C(F)(F)F|InChiKey: ZMPUACZRXUZAJD-QMMMGPOBSA-N|InChi: InChI=1S/C16H14ClF3N6O2/c1-8(28-2)14-10(7-22-13-6-12(17)25-26(13)14)24-15(27)23-9-3-4-21-11(5-9)16(18,19)20/h3-8H,1-2H3,(H2,21,23,24,27)/t8-/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 250 mg/mL (602.{{Cefditoren Pivoxil} medchemexpress|{Cefditoren Pivoxil} Bacterial|{Cefditoren Pivoxil} Technical Information|{Cefditoren Pivoxil} In stock|{Cefditoren Pivoxil} custom synthesis|{Cefditoren Pivoxil} Cancer} 74 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:|MLT-943 shows a high potency and selectivity in vitro. MLT-943 inhibits stimulated IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood).|In Vivo:|MLT-943 (oral gavage; 10 mg/kg; QD) prophylactic treatment in the rat collagen-induced arthritis model suppresses anti-collagen antibody production, fully prevents paw swelling, and normalizes joint histology scores in rat model.{{Maftivimab} web|{Maftivimab} Anti-infection|{Maftivimab} Purity & Documentation|{Maftivimab} In Vivo|{Maftivimab} manufacturer|{Maftivimab} Autophagy} MLT-943 (oral gavage; 5 mg/kg; QD; 10 consecutive days) effectively inhibits MALT1 protease activity and results in a progressive reduction in the frequency of Foxp3+CD25+ Treg cells in circulating CD4+ T cells, which was maximal after 7 days of treatment.PMID:24377291 And Discontinuation of MLT-943 treatment after day 10 leads to Treg frequency progressively returning to their original values within 4 days. Suboptimal doses of MLT-943 (0.1 and 0.5 mg/kg QD; p.o.) does not impact the Treg frequency. MLT-943 (oral gavage; 0, 5, 20 or 80 mg/kg/day; 4-13 weeks) causes a reduction in Treg and an increase in total T cell counts, in both 4- and 13-week rat toxicity studies at all dose levels. While a 4-Longer treatment induces severe immune-mediated pathology in multiple organs, with clinical onset starting around week 9 in rat. MLT-943 (p.o. admistration; 3 mg/kg; single dose) exhibits a good PK parameters in vivo. The Cmax values are 0.7 nM and 0.5 nM, respectively in rat and mice, respectively. And the F% are 86% and 50% in rat and mice, respective. For i.v. admistration the compound is formed in NMP:PEG200 (30/70); For p.o. admistration solution is formed in MC:Tween 80:Water (0.5:0.5:99) solution (Sourced from literature, for reference only).|Products are for research use only. Not for human use.|
