Zemocimig
Based on 1 Customer Validation
Zemocimig (NXT007) is an activated factor VIII mimetic antibody. Zemocimig binds to FX, FIXa and their activated forms to form a ternary complex, bridges FIXa and FX on the phospholipid surface, and restores intrinsic prothrombinase activity. Zemocimig induces thrombin generation, acts as a procoagulant, antifibrinolytic agent and hemostatic agent, and can shorten aPTT, increase fibrin deposition, correct clotting time, and reduce bleeding parameters. Zemocimig is applicable to the research of hemophilia A.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 95.59%
- CAS. Nr.: 2955620-21-8
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Ig(G4 - kappa_G4 - lambda2)
Human
F9a & F10
Zemocimig binds with high affinity to human and cynomolgus monkey FIX/FIXa and FX/FXa[1].
Zemocimig (31-150 nM) demonstrates activity equivalent to 40 IU/dL rhFVIII at 31 nM and 100 IU/dL rhFVIII at 150 nM[1].
Zemocimig strongly shortens APTT in FVIII-deficient hemophilia A plasma[1].
Zemocimig dose-dependently enhances thrombin generation activity in FXIa-triggered assays using FVIII-neutralized cynomolgus monkey plasma[1].
Zemocimig (0.1 nM) (as represented by its sequence-identical analogue zemocimig-SIA) exhibits high-affinity assembly of the FIXa/FX ternary complex with an apparent KD of 0.31 nM in a purified FX activation biochemical assay[2].
Zemocimig potently increases tissue factor-triggered peak height thrombin generation in platelet-rich and platelet-poor hemophilia A-like (FVIII-neutralized) plasma[3].
Zemocimig dose-dependently delays tissue plasminogen activator-mediated fibrinolysis in congenital hemophilia A plasma, and this effect correlates with thrombin generation[3].
Zemocimig (0.1, 1, 10, 100, 1000 μg/mL) potently increases tissue factor-triggered peak height thrombin generation in FVIII-neutralized human platelet-rich and platelet-poor plasma, reaching a maximum effect equivalent to 100 IU/dL porcine FVIII at 30-100 μg/mL, and is more potent than the comparator[4].
Zemocimig (0.1, 0.3, 1, 3, 10, 30, 100, 300 μg/mL) delays tPA-mediated fibrinolysis in severe human hemophilia A plasma with an EC50 of 1.7 μg/mL[4].
Zemocimig (0.005, 0.01, 0.05, 0.25, 1.25, 6.25, 37.5, 150 μg/mL (plasma equivalent); 30 min (anti-FVIII pre-incubation); 2 h (ROTEM measurement)) corrects clotting time and clotting kinetics in FVIII-neutralized human whole blood, with EC50 values of 24 ng/mL and 0.11 μg/mL, respectively[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Cmax | AUCinf | F |
|---|---|---|---|---|---|---|
| Cynomolgus Monkey[1] | 2 mg/kg | i.v. | 22.1 day | / | 834 μg/day/mL | / |
| Cynomolgus Monkey[1] | 0.02 mg/kg | s.c. | 21.9 day | 0.181 μg/mL | 6.84 μg/day/mL | 82.0 % |
| Cynomolgus Monkey[1] | 0.2 mg/kg | s.c. | 24.4 day | 1.95 μg/mL | 76.9 μg/day/mL | 92.2 % |
| Cynomolgus Monkey[1] | 2 mg/kg | s.c. | 19.6 day | 21.1 μg/mL | 704 μg/day/mL | 84.4 % |
Zemocimig (1-5 mg/kg) exhibits potent hemorrhage control efficacy in hemophilia A mice supplemented with human FIX/FX, with significant reductions in bleeding parameters observed at doses of 1 mg/kg and 5 mg/kg[3].
Zemocimig (2-20 mg/kg) shows no prothrombotic effects at doses of 2 mg/kg and 20 mg/kg in hemophilia A mice receiving human FIX/FX supplementation and subjected to ferric chloride-induced carotid artery injury[3].
Zemocimig (0.25-20 mg/kg; intravenous injection; single administration; administered 24 hours prior to tail amputation) controls acute bleeding in a mouse model of hemophilia A, and achieves a statistically significant reduction in bleeding time even at a dose as low as 1 mg/kg[4].
Zemocimig (2-20 mg/kg; single administration; 24 hours prior to injury) shows no prothrombotic properties in a ferric chloride-induced mouse arterial thrombosis model, even at high doses[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkey (male, 3-4 years old, 2.6-4.0 kg, acquired hemophilia A induced by anti-FVIII neutralizing antibody cyVIII-2236 followed by bleeding induction via muscle needling and subcutaneous abdomen exfoliation)[1]
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Dosage:0.0075 mg/kg; 0.025 mg/kg; 0.075 mg/kg; 0.6 mg/kg
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Administration:i.v.; single dose
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Result:Suppressed hemoglobin level decreases in a dose-dependent manner, with statistical significance vs vehicle achieved at doses ≥0.025 mg/kg.
Reduced bruised skin areas in a dose-dependent manner, with statistical significance vs vehicle achieved at doses ≥0.075 mg/kg.
Exerted hemostatic activity similar to twice-daily administration of 20 U/kg recombinant porcine FVIII at a single i.v. dose of 0.075 mg/kg.
Exhibited plasma concentrations ranging from 1.9 μg/mL (13 nM) on day 0 to 0.75 μg/mL (5.2 nM) on day 3 at 0.075 mg/kg, which is approximately 30-fold lower than plasma concentrations of emicizumab from a previous 3 mg/kg i.v. dose study.
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Animal Model:F8-knockout (8-12-week-old male, hemophilia A, transiently humanized with human FIX/hFX)[4]
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Dosage:0.25 mg/kg; 1 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.v.; single dose; 24 hours pre-tail vein transection
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Result:Reduced total bleeding time at doses of 1 mg/kg, 5 mg/kg, 10 mg/kg, and 20 mg/kg.
Shortened times to bleeding arrest compared to emicizumab.
Lowered rates of spontaneous rebleeding following wound rechallenge compared to emicizumab.
Achieved plasma concentrations ranging from ~10 μg/mL (1 mg/kg dose) to ~200 μg/mL (20 mg/kg dose).
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Animal Model:F8-knockout (10-12-week-old, hemophilia A, transiently humanized with human FIX/hFX, ferric chloride-induced carotid artery injury)[4]
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Dosage:2 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:single dose; 24 hours pre-injury
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Result:Did not cause >50% maximum blood flow reduction in any animal at doses corresponding to therapeutic and supratherapeutic plasma concentrations (~20-200 μg/mL).
Resulted in average maximum blood flow reduction <15% across all treatment groups.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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IgG4-kappa-lambda
ELISA, FACS, Functional assay
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Immobilized Coagulation factor IX/F9 Protein, Human (HEK293, HY-P70231) can bind Zemocimig, The ED50 for this effect is 111.6 ng/mL. -
Immobilized Coagulation Factor X/F10 Protein, Human (HEK293, HY-P7860) can bind Zemocimig, The ED50 for this effect is 766.2 ng/mL.
Chemical Information
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CAS. Nr. 2955620-21-8
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Appearance Liquid
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Color Colorless to light yellow
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SMILES
[Zemocimig]
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Synonyms
NXT007; RG6512; RO7589655
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Versand
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Data Sheet (267 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)
Verweise
[1]. Teranishi-Ikawa Y, et al. A bispecific antibody NXT007 exerts a hemostatic activity in hemophilia A monkeys enough to keep a nonhemophilic state. Journal of thrombosis and haemostasis : JTH. 2024 Feb;22(2):430-440. [Content Brief]
[4]. Locke M, et al. Next-generation FVIIIa-mimetic bispecific antibody NXT007: evaluation in preclinical models of hemostasis and thrombosis. Blood advances. 2026 Feb 24;10(4):1058-1067. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Zemocimig Related Classifications
HY-P991169 Related Classifications
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