NIBR0213 |
| カタログ番号GC18895 |
NIBR-0213 は、実験的自己免疫性脳脊髄炎に有効な強力かつ選択的な S1P1 アンタゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1233332-14-3
Sample solution is provided at 25 µL, 10mM.
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NIBR0213 is an orally bioavailable, potent, and selective antagonist of sphingosine-1-phosphate receptor-1 (S1P1) with IC50 values of 2.5 and 2.0 nM for the hS1P1 in a Ca2+ mobilization assay and GTPγS assay, respectively. [1] It is inactive at S1P2, S1P3, and S1P4 receptors (IC50s = >20, >10, and >10 uM, respectively in a Ca2+ mobilization assay). S1P1 plays a key role in the immune system, regulating lymphocyte egress from lymphoid tissues into the circulation.[2] In rats, NIBR0213 (30 mg/kg) reduces peripheral blood lymphocytes by 75-85% for up to 24 hours. [1] In a mouse model of experimental autoimmune encephalitis (EAE), it significantly reduces disease severity up to 26 days, when administered at 30 mg/kg twice per day for three days, then 60 mg/kg twice per day. However, in a rat model of adjuvant-induced arthritis, chronic administration of 30 mg/kg induces pulmonary damage and chronic lung inflammation.[3]
Reference:
[1]. Quancard, J., Bollbuck, B., Janser, P., et al. A potent and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. Chem. Biol. 19(9), 1142-1151 (2012).
[2]. Huwiler, A., Kolter, T., Pfeilschifter, J., et al. Physiology and pathophysiology of sphingolipid metabolism and signaling. Biochim. Biophys. Acta. 1485(2-3), 63-99 (2000).
[3]. Bigaud, M., Dincer, Z., Bollbuck, B., et al. Pathophysiological consequences of a break in S1P1-dependent homeostasis of vascular permeability revealed by S1P1 competitive antagonism. PLoS One 11(12), e0168252 (2016).
| Cas No. | 1233332-14-3 | SDF | |
| Chemical Name | N-[[3'-[[(1R)-1-(4-chloro-3-methylphenyl)ethyl]amino]-3,5-dimethyl[1,1'-biphenyl]-4-yl]carbonyl]-L-alanine | ||
| Canonical SMILES | CC1=C(Cl)C=CC([C@@H](C)NC2=CC(C3=CC(C)=C(C(N[C@@H](C)C(O)=O)=O)C(C)=C3)=CC=C2)=C1 | ||
| Formula | C27H29ClN2O3 | M.Wt | 465 |
| 溶解度 | 25mg/mL in DMSO, 25mg/mL in DMF, 25mg/mL in Ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1505 mL | 10.7527 mL | 21.5054 mL |
| 5 mM | 0.4301 mL | 2.1505 mL | 4.3011 mL |
| 10 mM | 0.2151 mL | 1.0753 mL | 2.1505 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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