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

CCR5 antagonist 2 (Compound 25) is a CCR5 antagonist with an IC50 of 8.34 nM. CCR5 antagonist 2 shows broad-spectrum anti-HIV-1 activities.

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CCR5 antagonist 2 Chemical Structure

CCR5 antagonist 2 Chemical Structure

CAS No. : 1800570-93-7

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CCR5 antagonist 2 Related Antibodies

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Description

CCR5 antagonist 2 (Compound 25) is a CCR5 antagonist with an IC50 of 8.34 nM. CCR5 antagonist 2 shows broad-spectrum anti-HIV-1 activities[1].

IC50 & Target[1]

CCR5

8.34 nM (IC50)

HIV-1

11 nM (EC50, TZM-bl cell)

In Vitro

CCR5 antagonist 2 (Compound 25) (48 h) shows excellent HIV-1 inhibitory activity with an EC50 of 0.011 ± 0.002 μM in TZM-bl cells[1].
CCR5 antagonist 2 (48 h) shows antiviral activities with an EC50 of 4.34 ± 1.61 nM against CCR5-tropic integrase inhibitor resistant strain HIV-1YU-2(G140S/Q148H) in TZM-bl cells[1].
CCR5 antagonist 2 shows HIV-1 inhibitory activity with EC50s of 7.82, 8.73, 12.61, 15.99 and 16.93 nM against HIV-1 strains KIZ001, YU-2, KIZ006, SF162 and Ba-L, respectively[1].

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

CCR5 antagonist 2 Related Antibodies
In Vivo

PK Properties of CCR5 antagonist 2 (Compound 25) 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 2 p.o. 10 49.5 ± 18.6 2.0 ± 0.0 10.3 ± 2.5 229 ± 92 283 ± 105 13.2 ± 4.2 – 15.7
i.v. 2 – – 1.60 ± 0.03 291 ± 75 298 ± 76 1.81 ± 0.04 117 ± 29

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

601.79

Formula

C32H45F2N5O2S
CAS No.
SMILES

CC1=NC2=C(N1[C@H]3C[C@H]4N(CC[C@@H](C5=CSC=C5)NC(C6CCC(F)(CC6)F)=O)[C@@H](C3)CC4)CCN(C2)C(C(C)C)=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 2 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 21800570-93-7CCRHIVCC chemokine receptorHuman immunodeficiency virusKIZ001YU-2KIZ006SF162Ba-LTZM-blPBMCsInhibitorinhibitorinhibit

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CCR5 antagonist 2
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