Natalizumab
Based on 3 publication(s) in Google Scholar
Natalizumab (AN100226; BG00002) is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d). It blocks the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4+ T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thus exerting anti-inflammatory and immunomodulatory activity. Natalizumab is used in the study of relapsing-remitting multiple sclerosis (RRMS) and also has applications in the study of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab can also prevent lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses.
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- Pureté: 99.10%
- CAS No.: 189261-10-7
- Masse moléculaire:146.19 kDa
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Natalizumab
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Activité biologique
Human IgG4 kappa
Human
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α4β1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
7 nM
Compound: Senktide
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Compound was evaluated for concentration-dependent and oscillatory increase in [Ca2+], caused by activation of hNK3 receptors in CHO cells
Compound was evaluated for concentration-dependent and oscillatory increase in [Ca2+], caused by activation of hNK3 receptors in CHO cells
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[PMID: 9871763] |
| CHO | IC50 |
>10000 nM
Compound: Senktide
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Displacement of [125I]-BH-SP from NK1 receptor (unknown origin) expressed in CHO cells by scintillation counter
Displacement of [125I]-BH-SP from NK1 receptor (unknown origin) expressed in CHO cells by scintillation counter
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10.1039/C4MD00514G |
| CHO | IC50 |
>10000 nM
Compound: Senktide
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Displacement of [125I]-NKA from NK2 receptor (unknown origin) expressed in CHO cells by scintillation counter
Displacement of [125I]-NKA from NK2 receptor (unknown origin) expressed in CHO cells by scintillation counter
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10.1039/C4MD00514G |
| CHO | IC50 |
0.056 μM
Compound: Senktide
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Displacement of [125I]His3, MePhe7 from human NK3R expressed in CHO cell membranes by scintillation counting
Displacement of [125I]His3, MePhe7 from human NK3R expressed in CHO cell membranes by scintillation counting
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[PMID: 25247671] |
| CHO | IC50 |
21 nM
Compound: Senktide
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Binding affinity towards human Tachykinin receptor 3 stably expressed in CHO cells using [125I][MePhe7]-NKB as radioligand
Binding affinity towards human Tachykinin receptor 3 stably expressed in CHO cells using [125I][MePhe7]-NKB as radioligand
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10.1016/0960-894X(95)00313-I |
| CHO | IC50 |
29 nM
Compound: Senktide
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Displacement of ([125I]His3-MePhe7)-NKB from NK3 receptor (unknown origin) expressed in CHO cells by scintillation counter
Displacement of ([125I]His3-MePhe7)-NKB from NK3 receptor (unknown origin) expressed in CHO cells by scintillation counter
|
10.1039/C4MD00514G |
Natalizumab (10 μg/mL, 2 h) reduced the adhesion of VLA-4-positive lymphoma cells (Raji, Karpas-422, etc.) to fibronectin by 75-95% and altered cell adhesion morphology[2].
Natalizumab (10 μg/mL in combination with rituximab) partially overcame the protective effect of bone marrow stromal cells on lymphoma B cells, mitigating resistance to apoptosis induced by Rituximab (HY-P9913) and cytotoxic drugs[2].
Natalizumab (30 μg/mL) slightly upregulated the expression of IL-2, IFN-γ, and IL-17 in activated CD4+ T cells, triggered MAPK/ERK phosphorylation, and downregulated CD49d surface expression[3].
Natalizumab (1 μg/mL) alone could not significantly inhibit the retention of CD4+ T cells or PBMCs in an inflammatory state BBB model (BLEC, HBMEC, etc.), requiring co-inhibition of β2-integrin for complete blockade[1].
Natalizumab (1 μg/mL) was ineffective in inhibiting shear-resistant retention of CD4+ Th1 cells when the molar ratio of ICAM-1 to VCAM-1 was 10:1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Natalizumab (170 μg/mouse; intravenous injection; single dose) only partially and transiently reduced the firm adhesion of human T cells to the activated BBB in a TNF-α-induced acute systemic inflammation model in female SJL mice, significantly reducing T cell rolling along the vessel wall but not affecting capture[4].
Natalizumab (0.625-2.5 mg/mouse; intravitreal injection; single dose; 21-day observation period) showed no functional or structural toxicity to the retina of New Zealand white rabbits at doses of 0.625-1.25 mg, with no significant changes in the amplitude and latency of a-wave and b-wave in electroretinography (ERG), but the 2.5 mg dose caused retinal dysfunction, with significantly reduced a-wave and b-wave amplitudes in ERG, and ultrastructural damage in the outer plexiform layer and inner nuclear layer[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG4 kappa
ELISA, FACS, Functional assay
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Flow cytometric analysis of 1X106 Jurkat cells with Natalizumab (HY-108831, 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 (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG4 (S228P) kappa Isotype Control (HY-P99003, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).
Chemical Information
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CAS No. 189261-10-7
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Appearance Liquid
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Masse moléculaire 146.19 kDa
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Color Colorless to light yellow
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SMILES
[Natalizumab]
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Mol Med
2024 Apr 22;30(1):54. PMID: 38649802 -
Pharmaceutics
LPX-TI641, a Tim3/4 Agonist, Induces Long-Term Immune Tolerance in Multiple Sclerosis Models. [Abstract]2025 Oct 30;17(11):1402. PMID: 41304740 -
Pureté et documentation
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Fiche technique (263 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)