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Cat. No. M8784
NIBR-0213 Structure
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

NIBR-0213 is an orally active, potent and S1P1-selective sphingosine 1-phosphate (S1P) receptor antagonist that blocks S1P1-selective ligand AUY954-induced Ca2+ mobilization (IC50 = 2.5 nM using human S1P1-transfected HeLa cells; IC50 >10 μM with human S1P2, S1P3, or S1P4 transfectants) and S1P-induced GTPγS recruitment (IC50 = 2.0/2.3/8.5 nM using membrane from human/murine/rat S1P1-transfected CHO cells; IC50 >10 μM with membrane from human S1P5 transfectant). NIBR-0213 induces long-lasting peripheral blood lymphocyte reduction in rats (EDmax = 1 mg/kg, ED50 = 0.2 mg/kg; p.o.) and exhibits therapeutic efficacy (30 mg/kg p.o; BID) in experimental autoimmune encephalomyelitis (EAE), a murine model of multiple sclerosis (MS), with no adverse effects to the animals.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 464.98
Formula C27H29ClN2O3
CAS Number 1233332-14-3
Purity >98%
Solubility DMSO: 2 mg/mL
Storage at -20°C

[1] Hao Jiang, et al. PET Study of Sphingosine-1-phosphate Receptor 1 Expression in Response to S. aureus Infection

[2] Simona Federica Spampinato, et al. Protective effect of the sphingosine-1 phosphate receptor agonist siponimod on disrupted blood brain barrier function

[3] Marc Bigaud, et al. Pathophysiological Consequences of a Break in S1P1-Dependent Homeostasis of Vascular Permeability Revealed by S1P1 Competitive Antagonism

[4] Jean Quancard, et al. A potent and selective S1P(1) antagonist with efficacy in experimental autoimmune encephalomyelitis

[5] Hideru Obinata, et al. Fine-tuning S1P therapeutics

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Abmole Inhibitor Catalog

Keywords: NIBR-0213 supplier, S1P Receptor, inhibitors

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