Cart
sales@molnova.com
JNJ-55308942
CAS No. 2166558-11-6
JNJ-55308942( JNJ55308942 )
Catalog No. M13460 CAS No. 2166558-11-6
JNJ-55308942 is a novel highly potent P2X7 antagonist with Ki of 1.0 and 6.5 nM for rat and human hP2X7, demonstrates significant activity against a panel of related P2X receptors (P2X1, P2X2, P2X3, P2X2/3, and P2X4; also shows insignificant inhibition of nine CYP isoforms (IC50>15 uM).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 180 | In Stock |
|
| 5MG | 163 | In Stock |
|
| 10MG | 264 | In Stock |
|
| 25MG | 510 | In Stock |
|
| 50MG | 721 | In Stock |
|
| 100MG | 1004 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | 2018 | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
-
Product NameJNJ-55308942
-
NoteResearch use only, not for human use.
-
Brief DescriptionJNJ-55308942 is a novel highly potent P2X7 antagonist with Ki of 1.0 and 6.5 nM for rat and human hP2X7, demonstrates significant activity against a panel of related P2X receptors (P2X1, P2X2, P2X3, P2X2/3, and P2X4; also shows insignificant inhibition of nine CYP isoforms (IC50>15 uM).
-
DescriptionJNJ-55308942 is a novel highly potent P2X7 antagonist with Ki of 1.0 and 6.5 nM for rat and human hP2X7, demonstrates significant activity against a panel of related P2X receptors (P2X1, P2X2, P2X3, P2X2/3, and P2X4; also shows insignificant inhibition of nine CYP isoforms (IC50>15 uM); exhibits excellent P2X7 receptor occupancy in the hippocampus of rats with low ED50 of 0.07 mg/kg and unbound plasma EC50 of 12 ng/mL, suppresses brain IL-1β release in vivo in freely moving rats challenged with the P2X7 agonist Bz-ATP; possesses good tolerability margins in preclinical species, as well as an acceptable cardiovascular safety profile in vivo.Epilepsy Phase 1 Clinical.
-
In Vitro——
-
In VivoAnimal Model:Sixteen male C57/BL6J mice Dosage:30?mg/kg Administration:P.o. (after an i.p. injection of LPS (0.8?mg/kg, i.p.))Result:Significantly attenuated the effect of LPS on FSC, CD45 surface expression and CD11b surface expression.Animal Model:Rat Dosage:P.o. (Pharmacokinetic Analysis)Administration:5 mg/kg Result:The F, Vss, CL, Cmax and AUC24h were 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively.
-
SynonymsJNJ55308942
-
PathwayMembrane Transporter/Ion Channel
-
TargetP2X Receptor
-
RecptorP2X Receptor
-
Research AreaNeurological Disease
-
IndicationEpilepsy
Chemical Information
-
CAS Number2166558-11-6
-
Formula Weight425.323
-
Molecular FormulaC17H12F5N7O
-
Purity>98% (HPLC)
-
SolubilityIn Vitro:?DMSO : 100 mg/mL (235.12 mM)
-
SMILES——
-
Chemical Name(S)-(3-fluoro-2-(trifluoromethyl)pyridin-4-yl)(1-(5-fluoropyrimidin-2-yl)-6-methyl-1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridin-5-yl)methanone
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Chrovian CC, et al. J Med Chem. 2018 Jan 11;61(1):207-223.
molnova catalog
related products
-
CE-224535
CE-224535 is a selective antagonist of P2X7 receptor. CE-224535 can be used in disease-modifying antirheumatic studies.
-
Opiranserin hydrochl...
Opiranserin (VVZ-149) hydrochloride is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. It shows antagonistic activity on rP2X3 (IC50=0.87 μM). It is development as an injectable agent for the treatment of postoperative pain.
-
PPADS tetrasodium
PPADS tetrasodiuma is a potent P2X receptor antagonist and inhibitor of the inverse mode of Na/Ca2? exchange in guinea pig airway smooth muscle and is neuroprotective against glutamate/NMDA toxicity.PPADS tetrasodiuma inhibits P2X1, P2X-2, P2X-3, and P2X- 5. 5.
