2. Anti-infection
  3. RSV
  4. CGR-51

CGR-51 is an orally active potent RSV fusion glycoprotein (F protein) inhibitor (EC50 = 19.4 nM against RSV A2 in HEp-2 cells). CGR-51 blocks RSV entry by binding to the F protein (KD = 0.1 μM) and inhibiting membrane fusion, a mechanism distinct from farnesyltransferase inhibition. CGR-51 selects for the K399N resistance mutation in the RSV F protein during in vitro passage. CGR-51 effectively suppresses RSV replication in a BALB/c mouse model of RSV infection. CGR-51 can be used for RSV infection research.

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CGR-51

CGR-51 Chemical Structure

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CGR-51 Related Antibodies

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Description

CGR-51 is an orally active potent RSV fusion glycoprotein (F protein) inhibitor (EC50 = 19.4 nM against RSV A2 in HEp-2 cells). CGR-51 blocks RSV entry by binding to the F protein (KD = 0.1 μM) and inhibiting membrane fusion, a mechanism distinct from farnesyltransferase inhibition. CGR-51 selects for the K399N resistance mutation in the RSV F protein during in vitro passage. CGR-51 effectively suppresses RSV replication in a BALB/c mouse model of RSV infection. CGR-51 can be used for RSV infection research[1].

In Vitro

CGR-51 (72 h) demonstrates potent, broad-spectrum activity against a panel of RSV strains (EC50 = 18.2 nM against A1540, EC50 = 46.5 nM against B9320, EC50 = 39.7 nM against B1) in HEp-2 Cells[1].
CGR-51 (72 h) exhibits a CC50 value of 19.4 μM and a superior selectivity index (SI = 1070.9) in HEp-2 Cells, compared to Lonafarnib (HY-15136), indicating a favorable safety profile[1].
CGR-51 (5 μM, 2-26 h) exerts its antiviral effect primarily by inhibiting RSV entry through suppression of viral fusion activity mediated by the RSV F protein[1].
CGR-51 (1-10 μM, 24 h) inhibits RSV infection in a dose-dependent manner by directly targeting the viral F protein, independently of farnesyltransferase inhibition and without inducing phospholipidosis[1].
CGR-51 shows substantially reduced activity against the K399N mutant virus, with 10.09- and 6.87-fold increases in EC50 and EC90, respectively, compared to the wild-type virus[1].

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

CGR-51 Related Antibodies
In Vivo

CGR-51 (20 and 40 mg/kg, p.o., BID for 4 days) dose-dependently mitigates RSV-induced pulmonary injury in BALB/c mice[1].

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

Animal Model: Female BALB/c mice (10 weeks old) intranasally inoculated with RSV A2[1]
Dosage: 20 and 40 mg/kg
Administration: p.o., BID for 4 days
Result: Exhibited antiviral efficacy comparable to the 40 mg/kg dose of Lonafarnib at 20 mg/kg.
Led to a substantial reduction in both pulmonary viral titers and RNA levels at 40 mg/kg.
Demonstrated effects similar to those observed in Lonafarnib (40 mg/kg) group, showing notable improvement in lung injury at 20 mg/kg.
Provided even greater alleviation of lung damage at 40 mg/kg.
Molecular Weight

656.81

Formula

C27H30Br2ClFN4O2
SMILES

O=C(N1CCC(C(F)C(N2CCC([C@@H]3C4=C(Br)C=C(Cl)C=C4CCC5=CC(Br)=CN=C53)CC2)=O)CC1)N
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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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CGR-51 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:

CGR-51CGR51CGR 51RSVRespiratory syncytial virusF proteinfarnesyltransferaseK399NHEp-2 CellsphospholipidosisRSV A2BALB/cInhibitorinhibitorinhibit

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