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Tocris/Maraviroc/3756/10/10 mg

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货号: 3756/10

品牌: Tocris

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Description: Selective CCR5 antagonist

Alternative Names: UK-427857

Chemical Name: 4,4-Difluoro-N-{(1S)-3-[3-(3-isopropyl- 5-methyl-4H-1,2,4-triazol-4-yl)- 8-azabicyclo[3.2.1]oct-8-yl]-1- phenylpropyl}cyclohexanecarboxamide

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Selective CCR5 antagonist; displays potent anti-HIV-1 activity. Prevents the interaction of HIV-1 gp120 and CCR5 (IC₅₀ = 6.4 nM), inhibiting HIV-1 entry. Exhibits antinociceptive effects in a rat model of neuropathic pain. Also inhibits CCL3 (MIP-1α) binding to CCR5. Orally bioavailable.

Licensing Information

Sold for research purposes under agreement from Viiv.

Compound Libraries

Maraviroc is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	513.67
Formula	C₂₉H₄₁F₂N₅O
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	376348-65-1
PubChem ID	483407
InChI Key	GSNHKUDZZFZSJB-ILVMPNSOSA-N
Smiles	O=C(C4CCC(F)(F)CC4)N[C@@H](CCN2C3CCC2CC(N5C(C)=NN=C5C(C)C)C3)C1=CC=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	38.53	75
	ethanol	51.37	100

Preparing Stock Solutions

The following data is based on the product molecular weight 513.67. Batch specific molecular weights may vary from batch to batch due to solvent 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	1.95 mL	9.73 mL	19.47 mL
5 mM	0.39 mL	1.95 mL	3.89 mL
10 mM	0.19 mL	0.97 mL	1.95 mL
50 mM	0.04 mL	0.19 mL	0.39 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Dorr et al (2005) Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity. Antimicrob.Agents Chemother. 49 4721 PMID: 16251317

Garcia-Perez et al (2011) New insights into the mechanisms whereby low molecular weight CCR5 ligands inhibit HIV-1 infection. J.Biol.Chem. 286 4978 PMID: 21118814

Kuritzkes et al (2008) Fresh from the pipeline - maraviroc. Nat.Rev.Drug Discov. 7 15 PMID:

Piotrowska et al (2016) Maraviroc reduces neuropathic pain through polarization of microglia and astroglia - Evidence from in vivo and in vitro studies. Neuropharmacology S0028-3908 30164 PMID: 27117708

Keywords: Maraviroc, supplier, UK-427857, HIV-1, gp120, CCR5, chemokine, receptors, ligands, selective, antagonists, HIV, Rantes, UK-427857, Antivirals, Chemokine, CC, Receptors, Chemokine, CC, Receptors, Tocris Bioscience

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