2. GPCR/G Protein Immunology/Inflammation Anti-infection
  3. CCR HIV
  4. CCR5 antagonist 3

CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities.

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CCR5 antagonist 3 Chemical Structure

CCR5 antagonist 3 Chemical Structure

CAS No. : 1800570-92-6

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CCR5 antagonist 3 Related Antibodies

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Description

CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities[1].

IC50 & Target[1]

CCR5

15.90 nM (IC50)

HIV-1

0.010 μM (EC50, In TZM-bl cells)

In Vitro

CCR5 antagonist 3 (Compound 26) (48 h) shows excellent HIV-1 inhibitory activity with an EC50 of 0.010 ± 0.004 μM in TZM-bl cells[1].
CCR5 antagonist 3 (48 h) shows antiviral activities with an EC50 of 2.71 ± 0.34 nM against CCR5-tropic integrase inhibitor resistant strain HIV-1YU-2(G140S/Q148H) in TZM-bl cells[1].
CCR5 antagonist 3 shows HIV-1 inhibitory activity with EC50s of 2.89, 5.26, 7.64, 9.96 and 19.01 nM against HIV-1 strains YU-2, KIZ001, SF162, Ba-L and KIZ006 respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CCR5 antagonist 3 Related Antibodies
In Vivo

PK Properties of CCR5 antagonist 3 (Compound 26) in SD Rats[1]

compd admin dose (mg/kg) Cmax (ng/mL) Tmax (h) T1/2 (h) AUC0–last (ng·h/mL) AUC0–∞ (ng·h/mL) MRT (h) CL (mL/min/kg) F (%)
CCR5 antagonist 3 p.o. 10 66.4 ± 64.0 2.67 ± 1.15 6.44 ± 2.10 249 ± 149 270 ± 145 9.16 ± 4.17 – 11.9
i.v. 2 – – 3.34 ± 1.55 420 ± 36 426 ± 34 2.43 ± 0.74 78.7 ± 6.6

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SD rats[1]
Dosage: 2 mg/kg and 10 mg/kg
Administration: Intravenous and oral administration (Pharmacokinetic Analysis)
Result: Displayed good PK profiles.
Molecular Weight

573.74

Formula

C30H41F2N5O2S
CAS No.
SMILES

CC(N(C1)CCC2=C1N=C(C)N2[C@@H]3C[C@H]4N(CC[C@@H](C5=CSC=C5)NC(C6CCC(F)(CC6)F)=O)[C@@H](C3)CC4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CCR5 antagonist 3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CCR5 antagonist 31800570-92-6CCRHIVCC chemokine receptorHuman immunodeficiency virusKIZ001YU-2KIZ006SF162Ba-LTZM-blPBMCsInhibitorinhibitorinhibit

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