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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $39 | In Stock | |
5 mg | $77 | In Stock | |
10 mg | $113 | In Stock | |
25 mg | $229 | In Stock | |
50 mg | $340 | In Stock | |
1 mL x 10 mM (in DMSO) | $117 | In Stock |
Description | NIBR-0213, a potent and selective S1P(1) antagonist, has efficacy in experimental autoimmune encephalomyelitis. |
Targets&IC50 | S1P1:2.5 nM(Ca2+ mobilization), S1P1:2.3 nM(GTPγ35S,rat), S1P1:8.5 nM(GTPγ35S,mouse), S1P1:2.0 nM(GTPγ35S,human) |
In vitro | In Ca2+?mobilization assays, NIBR-0213 displayed an inhibitory activity on hS1P1?with an IC50?of 2.5?nM whereas it was inactive (IC50?> 10?μM) on S1P2, S1P3, and S1P4. In GTPγ35S assays, NIBR-0213 displayed potent and comparable potency on human and rat S1P1?(IC50?of 2.0?nM and 2.3?nM, respectively), whereas on mouse S1P1?a slightly reduced IC50?of 8.5?nM was?measured. NIBR-0213 showed an ~3,000-fold selectivity against human S1P5?in the GTPγ35S assay (Figure?3A). On S1P4, a weak agonistic activity was detected with an EC50?of 245?nM. Schild plot analysis indicated that NIBR-0213 is a competitive S1P1?antagonist with a calculated Kd?of 0.37?± 0.031?nM[2]. |
In vivo | NIBR-0213 increased in a dose-dependent manner the leakage of?plasma proteins?into lung parenchyma, as measured by the increase in EBD in lung tissues at 6?hr posttreatment (time of Emax on PBL). A maximum of 4–5-fold EBD increase versus vehicle controls was observed with 0.3?mg/kg. An ED50?of ~0.1?mg/kg could be estimated, i.e., in the range of the ED50?for the effects on PBL counts[2]. NIBR-0213 given orally at 30 mg/kg to rats reduced the PBL counts by 75%–85% within 14 hr and maintained this effect up to 24 hr posttreatment[2]. |
Alias | NIBR 0213 |
Molecular Weight | 464.98 |
Formula | C27H29ClN2O3 |
Cas No. | 1233332-14-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/ml (118.28 mM) ![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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