Apitegromab
Based on 1 Customer Validation
Apitegromab (SRK-015) is an anti-promyostatin monoclonal antibody. Apitegromab can be used for the research of neuromuscular disease including spinal muscular atrophy.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 2278276-46-1
- Molecular Weight:145.06 kDa
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Human IgG4 lambda
Human
GDF8/Myostatin
Apitegromab (IC50: Human 286 nM, Cynomolgus 626 nM, Rat 178 nM, 16 h) effectively inhibits promyostatin activation, with species-dependent potency differences[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Note | Clearance (CL) | Tmax | AUC |
|---|---|---|---|---|---|---|
| Cynomolgus Monkey[2] | 10 mg/kg | i.v. | / | 369 μg/mL | 1 h | 30400 μg·h/mL |
| Cynomolgus Monkey[2] | 100 mg/kg | i.v. | / | 2560 μg/mL | 1 h | 240000 μg·h/mL |
| Cynomolgus Monkey[2] | 30 mg/kg | i.v. | / | 876 μg/mL | 1 h | 77200 μg·h/mL |
| Rat[2] | 10 mg/kg | i.v. | Age: 6-8 weeks | 213 μg/mL | 1.0 h | 16200 μg·h/mL |
| Rat[2] | 100 mg/kg | i.v. | Age: 6-8 weeks | 2360 μg/mL | 1 h | 170000 μg·h/mL |
| Rat[2] | 30 mg/kg | i.v. | Age: 6-8 weeks | 695 μg/mL | 1 h | 51100 μg·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult cynomolgus monkeys (32-48 months)[2]
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Dosage:10, 30, 100 mg/kg
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Administration:Intravenous bolus (IV bolus), once weekly for 4 weeks
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Result:Did not cause treatment-related adverse effects, increased gastrocnemius and biceps brachii mass (5-25%), but did not exhibit dose dependency, and did not lead to significant histopathological changes or cardiac electrophysiological abnormalities.
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Animal Model:Sprague Dawley rats: adult group (6-8 weeks) or juvenile group (postnatal day 21)[2]
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Dosage:10, 30, 100, 300 mg/kg
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Administration:Intravenous bolus (IV bolus), once weekly for 4 weeks (adult group), 7 weeks (juvenile group) or 26 weeks (adult group)
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Result:Increased body weight independently of food intake, enhanced skeletal muscle mass (biceps brachii and gastrocnemius) by 3-32%, and caused minor clinical chemistry changes (mild increase in total protein and globulin), which were mostly reversible (adult group, administration for 4 weeks). increased muscle mass by 15-33%, induced mild muscle fiber hypertrophy (histological analysis), and caused minor hematological changes without significant toxicity; it did not produce adverse effects on cardiovascular, neurological, or reproductive systems (adult group, administration for 26 weeks). increased body weight (significant in females) without impacting growth and development, enhanced skeletal muscle mass (biceps brachii and gastrocnemius) by 13-28%, and did not cause neurobehavioral abnormalities (acoustic startle, locomotor activity, Morris water maze); it had no effects on sperm quality or fertility, indicating normal reproductive function (juvenile group).
| 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 lambda
ELISA, FACS, Functional assay
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Immobilized hu-Latentmyostatin-His can bind Apitegromab. The EC50 for this effect is 25.3 ng/mL. -
Flow cytometric analysis of 1X106 HeLa cells with Apitegromab (HY-P99441, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. AF 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 kappa (HY-P99003, blue) was used as the isotype control.
Chemical Information
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CAS No. 2278276-46-1
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Appearance Liquid
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Molecular Weight 145.06 kDa
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Color Colorless to light yellow
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SMILES
[Apitegromab]
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Synonyms
SRK-015
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (261 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)
References
[1]. Doreen Barrett, et al. A Randomized Phase 1 Safety, Pharmacokinetic and Pharmacodynamic Study of the Novel Myostatin Inhibitor Apitegromab (SRK-015): A Potential Treatment for Spinal Muscular Atrophy. Adv Ther. 2021 Jun;38(6):3203-3222. [Content Brief]
[2]. Welsh BT, et al. Preclinical Safety Assessment and Toxicokinetics of Apitegromab, an Antibody Targeting Proforms of Myostatin for the Treatment of Muscle-Atrophying Disease. Int J Toxicol. 2021 Jul-Aug;40(4):322-336. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Apitegromab Related Classifications
HY-P99441 Related Classifications
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