CP-481715

    WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H524803

CAS#: 212790-31-3

Description: CP 481715 a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases. P-481,715 binds to human CCR1 with a Kd of 9.2 nm. and displaces 125I-labeled CCL3 from CCR1-transfected cells with an IC50 of 74 nm. CP-481,715 fully blocks the ability of CCL3 and CCL5 to stimulate receptor signaling (guanosine 5'-O-(thiotriphosphate) incorporation; IC50 = 210 nm), calcium mobilization (IC50 = 71 nm), monocyte chemotaxis (IC50 = 55 nm), and matrix metalloproteinase 9 release (IC50 = 54 nm). CP-481,715 retains activity in human whole blood, inhibiting CCL3-induced CD11b up-regulation and actin polymerization (IC50 = 165 and 57 nm, respectively) on monocytes. CP-481,715 inhibits cell infiltration and inflammatory responses in human CCR1 transgenic mice.

Chemical Structure

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CP-481715
CAS# 212790-31-3
Instruction

Theoretical Analysis

Hodoodo Cat#: H524803
Name: CP-481715
CAS#: 212790-31-3
Chemical Formula: C26H31FN4O4
Exact Mass: 482.23
Molecular Weight: 482.550
Elemental Analysis: C, 64.71; H, 6.48; F, 3.94; N, 11.61; O, 13.26

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: CP 481715; CP481715; CP-481715; CP-481,715; CP 481,715; CP481,715.

IUPAC/Chemical Name: N-((2S,3S,5R)-5-carbamoyl-1-(3-fluorophenyl)-3,8-dihydroxy-8-methylnonan-2-yl)quinoxaline-2-carboxamide

InChi Key: YEQJVHQCUDMXFG-FHZYATBESA-N

InChi Code: InChI=1S/C26H31FN4O4/c1-26(2,35)11-10-17(24(28)33)14-23(32)21(13-16-6-5-7-18(27)12-16)31-25(34)22-15-29-19-8-3-4-9-20(19)30-22/h3-9,12,15,17,21,23,32,35H,10-11,13-14H2,1-2H3,(H2,28,33)(H,31,34)/t17-,21+,23+/m1/s1

SMILES Code: O=C(C1=NC2=CC=CC=C2N=C1)N[C@@H](CC3=CC=CC(F)=C3)[C@@H](O)C[C@H](C(N)=O)CCC(C)(O)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:

Preparing Stock Solutions

The following data is based on the product molecular weight 482.55 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.

Recalculate based on batch purity %
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:

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1: Gilchrist A, Gauntner TD, Fazzini A, Alley KM, Pyen DS, Ahn J, Ha SJ, Willett A, Sansom SE, Yarfi JL, Bachovchin KA, Mazzoni MR, Merritt JR. Identifying bias in CCR1 antagonists using radiolabelled binding, receptor internalization, β-arrestin translocation and chemotaxis assays. Br J Pharmacol. 2014 Nov;171(22):5127-38. doi: 10.1111/bph.12835. PubMed PMID: 24990525; PubMed Central PMCID: PMC4253460.

2: Gladue RP, Brown MF, Zwillich SH. CCR1 antagonists: what have we learned from clinical trials. Curr Top Med Chem. 2010;10(13):1268-77. Review. PubMed PMID: 20536425.

3: Borregaard J, Skov L, Wang L, Ting N, Wang C, Beck LA, Sonne J, Clucas A. Evaluation of the effect of the specific CCR1 antagonist CP-481715 on the clinical and cellular responses observed following epicutaneous nickel challenge in human subjects. Contact Dermatitis. 2008 Oct;59(4):212-9. doi: 10.1111/j.1600-0536.2008.01365.x. PubMed PMID: 18844696.

4: Clucas AT, Shah A, Zhang YD, Chow VF, Gladue RP. Phase I evaluation of the safety, pharmacokinetics and pharmacodynamics of CP-481,715. Clin Pharmacokinet. 2007;46(9):757-66. PubMed PMID: 17713973.

5: Gladue RP, Cole SH, Roach ML, Tylaska LA, Nelson RT, Shepard RM, McNeish JD, Ogborne KT, Neote KS. The human specific CCR1 antagonist CP-481,715 inhibits cell infiltration and inflammatory responses in human CCR1 transgenic mice. J Immunol. 2006 Mar 1;176(5):3141-8. PubMed PMID: 16493073.

6: Gladue RP, Tylaska LA, Brissette WH, Lira PD, Kath JC, Poss CS, Brown MF, Paradis TJ, Conklyn MJ, Ogborne KT, McGlynn MA, Lillie BM, DiRico AP, Mairs EN, McElroy EB, Martin WH, Stock IA, Shepard RM, Showell HJ, Neote K. CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases. J Biol Chem. 2003 Oct 17;278(42):40473-80. Epub 2003 Aug 7. PubMed PMID: 12909630.