WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H522415
CAS#: 300816-15-3
Description: RS-504393 is an extremely selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 µM for inhibition of human recombinant CCR2b and CCR1 receptors respectively). It inhibits MCP-1 chemotaxis (IC50 = 330 nM) and ischemia-reperfusion injury in kidneys.
Hodoodo Cat#: H522415
Name: RS-504393
CAS#: 300816-15-3
Chemical Formula: C25H27N3O3
Exact Mass: 417.21
Molecular Weight: 417.510
Elemental Analysis: C, 71.92; H, 6.52; N, 10.06; O, 11.50
Synonym: RS504393; RS 504393; RS-504393.
IUPAC/Chemical Name: 6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one
InChi Key: ODNICNWASXKNNQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H27N3O3/c1-17-8-9-22-20(16-17)25(31-24(29)27-22)11-14-28(15-12-25)13-10-21-18(2)30-23(26-21)19-6-4-3-5-7-19/h3-9,16H,10-15H2,1-2H3,(H,27,29)
SMILES Code: CC1=CC2=C(C=C1)NC(=O)OC23CCN(CC3)CCC4=C(OC(=N4)C5=CC=CC=C5)C
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 417.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Lu W, Tang Y, Zhang Z, Zhang X, Yao Y, Fu C, Wang X, Ma G. Inhibiting the mobilization of Ly6C(high) monocytes after acute myocardial infarction enhances the efficiency of mesenchymal stromal cell transplantation and curbs myocardial remodeling. Am J Transl Res. 2015 Mar 15;7(3):587-97. eCollection 2015. PubMed PMID: 26045897; PubMed Central PMCID: PMC4448197.
2: Wang A, Wang Z, Cao Y, Cheng S, Chen H, Bunjhoo H, Xie J, Wang C, Xu Y, Xiong W. CCL2/CCR2-dependent recruitment of Th17 cells but not Tc17 cells to the lung in a murine asthma model. Int Arch Allergy Immunol. 2015;166(1):52-62. doi: 10.1159/000371764. Epub 2015 Mar 4. PubMed PMID: 25765592.
3: Carmo AA, Costa BR, Vago JP, de Oliveira LC, Tavares LP, Nogueira CR, Ribeiro AL, Garcia CC, Barbosa AS, Brasil BS, Dusse LM, Barcelos LS, Bonjardim CA, Teixeira MM, Sousa LP. Plasmin induces in vivo monocyte recruitment through protease-activated receptor-1-, MEK/ERK-, and CCR2-mediated signaling. J Immunol. 2014 Oct 1;193(7):3654-63. doi: 10.4049/jimmunol.1400334. Epub 2014 Aug 27. PubMed PMID: 25165151.
4: Wakida N, Kiguchi N, Saika F, Nishiue H, Kobayashi Y, Kishioka S. CC-chemokine ligand 2 facilitates conditioned place preference to methamphetamine through the activation of dopamine systems. J Pharmacol Sci. 2014;125(1):68-73. Epub 2014 Apr 19. PubMed PMID: 24748435.
5: Zhu X, Cao S, Zhu MD, Liu JQ, Chen JJ, Gao YJ. Contribution of chemokine CCL2/CCR2 signaling in the dorsal root ganglion and spinal cord to the maintenance of neuropathic pain in a rat model of lumbar disc herniation. J Pain. 2014 May;15(5):516-26. doi: 10.1016/j.jpain.2014.01.492. Epub 2014 Jan 23. PubMed PMID: 24462503.
6: Pevida M, González-Rodríguez S, Lastra A, García-Suárez O, Hidalgo A, Menéndez L, Baamonde A. Involvement of spinal chemokine CCL2 in the hyperalgesia evoked by bone cancer in mice: a role for astroglia and microglia. Cell Mol Neurobiol. 2014 Jan;34(1):143-56. PubMed PMID: 24122510.
7: Liu S, Zhang L, Wu Q, Wu Q, Wang T. Chemokine CCL2 induces apoptosis in cortex following traumatic brain injury. J Mol Neurosci. 2013 Nov;51(3):1021-9. doi: 10.1007/s12031-013-0091-8. Epub 2013 Aug 11. PubMed PMID: 23934512.
8: Arms L, Girard BM, Malley SE, Vizzard MA. Expression and function of CCL2/CCR2 in rat micturition reflexes and somatic sensitivity with urinary bladder inflammation. Am J Physiol Renal Physiol. 2013 Jul 1;305(1):F111-22. doi: 10.1152/ajprenal.00139.2013. Epub 2013 Apr 17. PubMed PMID: 23594826; PubMed Central PMCID: PMC3725675.
9: Pevida M, Lastra A, Hidalgo A, Baamonde A, Menéndez L. Spinal CCL2 and microglial activation are involved in paclitaxel-evoked cold hyperalgesia. Brain Res Bull. 2013 Jun;95:21-7. doi: 10.1016/j.brainresbull.2013.03.005. Epub 2013 Apr 2. PubMed PMID: 23562605.
10: Pevida M, González-Rodríguez S, Lastra A, Hidalgo A, Menéndez L, Baamonde A. CCL2 released at tumoral level contributes to the hyperalgesia evoked by intratibial inoculation of NCTC 2472 but not B16-F10 cells in mice. Naunyn Schmiedebergs Arch Pharmacol. 2012 Nov;385(11):1053-61. doi: 10.1007/s00210-012-0787-2. Epub 2012 Sep 14. PubMed PMID: 22976830.
