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| カタログ番号 | HB010036 |
|---|---|
| 説明 |
Anti-REGN5381 Reference Antibody (Imelciment, RUO) (HB010036) is a human monoclonal antibody detecting NPR1/NPR-A. Expressed in Mammalian cells.
|
| 種反応性 | Human |
| アプリケーション | ELISA, Bioactivity: FCM, Functional assay, Research in vivo |
| 宿主種 | Human |
| クローン性 | Monoclonal |
| アイソタイプ | Immunoglobulin (H-gamma4_L-kappa)_G4hCH2CH3 |
| 生物学的活性 | Vixticibart specifically binds to human and monkey natriuretic peptide receptor 1 extracellular domain proteins, with no cross-reactivity to mouse natriuretic peptide receptor 1, natriuretic peptide receptor 2, or natriuretic peptide receptor 3, and does not interfere with atrial natriuretic peptide binding to human natriuretic peptide receptor 1 [1]. Vixticibart (10 -12 to 10 -6 M; under conditions supporting binding) dose-dependently binds to human and monkey natriuretic peptide receptor 1-expressing HEK293 cells, with enhanced binding in the presence of atrial natriuretic peptide or brain natriuretic peptide, and EC 50 values ranging from 2.27 to 5.69 nM [1]. Vixticibart (10 -15 to 10 -5 M) dose-dependently agonizes human and monkey natriuretic peptide receptor 1 in a calcium flux bioassay, with EC 50 values ranging from 42.5 to 82.2 nM, and achieves maximum activation comparable to natriuretic peptide ligands at high concentrations [1]. Vixticibart (10 -14 to 10 -5 M) dose-dependently activates human natriuretic peptide receptor 1 to induce cGMP accumulation in HEK293 cells, acts as a partial agonist relative to natriuretic peptide ligands, and shows enhanced activation in the presence of low concentrations of atrial natriuretic peptide or brain natriuretic peptide [1]. Vixticibart (molar excess; overnight at 4°C) binds to the N-terminal domain of human NPR1 dimers, stabilizing an active conformation in the presence of atrial natriuretic peptide and an active-like conformation in the absence of atrial natriuretic peptide, which drives downstream signaling [1]. Vixticibart (1-50 mg/kg; s.c.; single dose) induces a 10-15 mm Hg reduction in systolic blood pressure in normotensive NPR1 hu/hu mice, with dose-dependent duration of effect lasting up to 28 days for the 50 mg/kg dose [1]. Vixticibart (25 mg/kg; i.v. |
| 発現システム | Mammalian cells |
| 性質 | Recombinant |
| ターゲット | Vixticibart |
| エンドトキシンレベル | < 10 EU/mg as determined by LAL method. |
| 純度 | >95% as determined by SDS-PAGE. |
| 精製 | Protein A/G purified from cell culture supernatant. |
| アクセッション番号 | CAS: 2845128-05-2 |
| 形態 | Liquid |
| 保存バッファー | 0.01M PBS pH 7.4. データシートのハードコピーまたはロット固有のCOAに記載された具体的なバッファー情報を参照してください。 |
| 安定性と保存 | Use a manual defrost freezer and avoid repeated freeze thaw cycles. Store at 2 to 8°C for frequent use. Store at -20 to -80°C for twelve months from the date of receipt. |
| 別名 | Idiotypic, 2845128-03-0 |
| 背景 | Atrial natriuretic peptide receptor 1 (NPR1/NPR-A) is a ~118 kDa protein. Receptor for the atrial natriuretic peptide NPPA/ANP and the brain natriuretic peptide NPPB/BNP which are potent vasoactive hormones playing a key role in cardiovascular homeostasis. Plays an essential role in the regulation of endothelial cell senescence and vascular aging. Upon activation by ANP or BNP, stimulates the production of cyclic guanosine monophosphate (cGMP) that promotes vascular tone and volume homeostasis by activation of protein kinase cGMP-dependent 1/PRKG1 and subsequently PRKAA1, thereby controlling blood pressure and maintaining cardiovascular homeostasis. 1. Liu, S. et al. (2025) Nature structural & molecular biology 32, 469-478. PMID: 39543315 2. Long, C. et al. (2022) Aging cell 21, e13699. PMID: 36016499 |
| 参考文献 | 1. Dunn ME, et al. Agonist antibody to guanylate cyclase receptor NPR1 regulates vascular tone. Nature. 2024;633(8030):654-661. [HB010036] 2. Dunn M, et al. A novel agonist antibody to membrane-bound guanylate cyclase receptor, natriuretic peptide receptor 1, induces sustained vasodilation[J]. 2023. [HB010036] 3. Kithcart A P, et al. Effects of REGN5381, a natriuretic peptide receptor 1 agonist antibody, in hypertensive mouse models and mildly hypertensive but otherwise healthy adults in a phase 1 first-in-human study[J]. Journal of the American College of Cardiology, 2024, 83(13_Supplement): 1706-1706. [HB010036] |
| 注意事項 | For research use only. Not suitable for clinical or therapeutic use. |
| Isotype Control | Human IgG4 (S228P) Recombinant Isotype Control Antibody (13R4) (HP298207) |
SDS-PAGE for Research Grade Imelciment
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