1. GPCR/G Protein Neuronal Signaling
  2. CGRP Receptor
  3. Fremanezumab

Fremanezumab  (Synonyms: TEV-48125; LBR-101; PF-04427429; RN-307)

Cat. No.: HY-P99019 Purity: 95.00%
Technical Support

Fremanezumab (TEV-48125) is a humanized lgG2 monoclonal antibody that selectively and potently binds to calcitonin gene related peptide (CGRp) (IC50 values = 7.943 nM). Fremanezumab binds to mouse CGRP with an IC50 value of 19.6 nM. Fremanezumab counteracts anti-inflammatory effects of CGRP in vitro, including CGRP-mediated inhibition of LPS (HY-D1056)-induced microglial activation. Fremanezumab selectively inhibits the activation of Aδ meningeal nociceptors by cortical spreading depression (CSD) in rats. Fremanezumab can be used for the study of inflammation and chronic migraine.

For research use only. We do not sell to patients.

CAS No. : 1655501-53-3

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Description

Fremanezumab (TEV-48125) is a humanized lgG2 monoclonal antibody that selectively and potently binds to calcitonin gene related peptide (CGRp) (IC50 values = 7.943 nM). Fremanezumab binds to mouse CGRP with an IC50 value of 19.6 nM. Fremanezumab counteracts anti-inflammatory effects of CGRP in vitro, including CGRP-mediated inhibition of LPS (HY-D1056)-induced microglial activation. Fremanezumab selectively inhibits the activation of Aδ meningeal nociceptors by cortical spreading depression (CSD) in rats. Fremanezumab can be used for the study of inflammation and chronic migraine[1][2][3].

IC50 & Target

CALCA/CGRP

In Vitro

Fremanezumab (10 μM, 6 h) counteracts the concentration-dependent inhibitory effects of mouse CGRP on LPS (HY-D1056)-induced increases in IL1β, IL6, and IL12 transcripts in primary cultures of C57Bl mouse microglia, but does not alter microglia activation alone upon LPS incubation[1].
Fremanezumab (72 h) prevents the concentration-dependent inhibition of proliferation of splenocytes derived from day 30 MOG35-55-immunized NOD by mouse CGRP, but does not alter lymphocyte proliferation alone[1].
Fremanezumab (1-100 ng, 1 h) reduces immunodetection of human and mouse CGRP with IC50s of 7.94 nM and 19.6 nM, respectively[1].
Fremanezumab ((0.00001-1 μM) significantly inhibits the vasodilatory effects induced by human αCGRP, rat αCGRP and the metabolically stable CGRP analog SAX in rat cerebral basilar artery segments and reduces the potency of CGRP (pEC50 from 8.0 to 6.3) and SAX (pEC50 from 7.2 to 6.2)[2]

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

In Vivo

Fremanezumab (100 mg/kg, s.c., once every 2 weeks) shows no impact on disease evolution, survival, spinal cord neurodegeneration, or innate/adaptive immune responses in NOD mice[1].
Fremanezumab (30 mg/kg, i.v., once) selectively inhibits the activation of Aδ meningeal nociceptors by cortical spreading depression (CSD) in anesthetized male rats[3].

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

Animal Model: Male Sprague-Dawley rats (225-325 g)[3]
Dosage: 30 mg/kg
Administration: i.v., once
Result: Achieved a significantly lower activation rate of Aδ meningeal nociceptors by CSD.
Showed a significant increase in the firing rate of activated C-fiber meningeal nociceptors.
Clinical Trial
Molecular Weight

145.5 kDa

CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Fremanezumab]

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Format
  • Human IgG2 kappa
Biological Activity
  • Flow cytometric analysis of 1X106 A549 cells with Fremanezumab (HY-P99019, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Fluor 488-conjugated AffiniPure Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG2 kappa (HY-P99002, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).
Purity & Documentation

Purity: 95.00%

References
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  • 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.

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