Sotatercept (mIgG2a)
Based on 1 publication(s) in Google Scholar
Sotatercept (mIgG2a) (RAP-011), the murine homolog of Sotatercept (ACE-011) (HY-P99590), is a soluble activin receptor type IIA (ActRIIA) ligand trap. Sotatercept (mIgG2a) inhibits the binding of activin A and other members of the TGF-β superfamily (such as Activin A/B, GDF11 and BMP9/10) to their receptors by combining and neutralizing them, thereby regulating cell proliferation and differentiation. Sotatercept (mIgG2a) mainly inhibits the SMAD2/3 signaling pathway, and can be used in various diseases such as chronic kidney disease. Sotatercept (mIgG2a) reduces the expression of erythropoietic hepcidin (ERFE), regulates iron metabolism, and promotes red blood cell production. Sotatercept (mIgG2a) has a dual effect of promoting bone formation (anabolic) and inhibiting bone resorption (catabolic).
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- Reinheit: 99.93%
- Molecular Weight:79.67 kDa
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
-351671.png "Click to View Experimental Validation Results")
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Sotatercept (mIgG2a)
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Biologische Aktivität
Sotatercept (mIgG2a) (0.05 g/L, 1 h- 5 d) inhibits SMAD2 phosphorylation and ERFE expression, induces nuclear translocation of the transcription factor GATA1 and restores gene expression of erythroid markers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 cells
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Concentration:0.05 g/L with 50 ng/mL GDF11
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Incubation Time:5 d
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Result:Significantly upregulated the erythroid differentiation markers (such as KLF1, ABCB6, etc.).
Upregulated the anti-apoptotic gene BCL2 and downregulated the pro-apoptotic genes BAX/BAD.
Significantly reduced the expression of mRNA ERFE.
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Cell Line:K562 cells
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Concentration:0.05 g/L with 50 ng/mL GDF11
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Incubation Time:0.5, 1, 2 h
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Result:Significantly inhibited the phosphorylation of SMAD2 induced by GDF1.
Promoted the nuclear translocation of GATA1, accompanied by an increase in nuclear expression of HSP70 and a decrease in nuclear expression of SMAD4.
Significantly reduced the expression of ERFE protein.
Sotatercept (mIgG2a) (30 mg/kg, i.p., once daily for 10 days) shows a significant effect in stimulating red blood cell production in Hamp transgenic mice, while avoiding the common problem of iron depletion that occurs in Erythropoietin (HY-P70409) treatment[3].
Sotatercept (mIgG2a) (10 mg/kg, s.c., twice a week for 6 weeks) protects against vascular calcification and renal fibrosis in chronic kidney disease (CKD) mice model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Closed femoral fracture surgery established in 8-week male Wistar rats[2]
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Dosage:0.6 mg/kg biw (x 2 doses) + 0.35 mg/kg biw (x 3 doses); 0.18 mg/kg biw (x2 doses) + 0.1 mg/kg biw (x 7 doses) and 10mg/kg biw (x 12 doses)
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Administration:Subcutaneous injection (s.c.), twice a week for 2-6 weeks
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Result:Significantly increased callus length and bone volume at high-dose RAP-011 (10mg/kg biw), but the quality of the newly formed bone tissue was relatively low, and the improvement in mechanical properties was limited.
Demonstrated certain anabolic effects at low-dose pulsed administration.
No obvious effect at continuous low-dose administration.
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Animal Model:Iron-deficiency anemia model established in C57BL/6 mice and in hepcidin antimicrobial peptide over expressing mice (Tg-Hamp mice)[3]
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Dosage:30 mg/kg
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Administration:Intraperitoneal injection (i.p.), once daily for 10 days
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Result:Significantly increase the hemoglobin concentration in both wild-type and Tg-Hamp mice (better).
Promoted the production of red blood cells while not causing excessive depletion of iron reserves.
Significantly increased the proportion of late erythroid precursor cells (the CD44low population).
Did not change the expression level of Hamp.
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Animal Model:CKD that stimulated atherosclerotic calcification model established in high fat fed ldlr−/− mice[4]
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Dosage:10 mg/kg
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Administration:Subcutaneous injection (s.c.), twice weekly for 6 weeks
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Result:Reduced the calcium content and calcium deposits in the aortal.
Increased the markers of vascular smooth muscle (sm22α, αSMA) and reduced osteogenic markers (Runx2, alkaline phosphatase).
Restored the ActRIIA signal and regulated the Wnt signal.
Inhibited fibrosis mediated by Smad, increased the expression of klotho and downregulated the Wnt/Dkk1 signaling pathway.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
ELISA, FACS, Functional assay
Chemical Information
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Appearance Liquid
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Molecular Weight 79.67 kDa
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Color Colorless to light yellow
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SMILES
[Sotatercept (mIgG2a)]
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Synonyms
RAP-011
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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.
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Endothelial C-type natriuretic peptide/guanylyl cyclase-B signaling prevents pulmonary arterial hypertension. [Abstract]2026 Mar 17;17(1):2331. PMID: 41844596
Reinheit & Dokumentation
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Data Sheet (267 KB)
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SDS (251 KB)
- English - EN (251 KB)
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- 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]. De Rosa G, et al. RAP-011 Rescues the Disease Phenotype in a Cellular Model of Congenital Dyserythropoietic Anemia Type II by Inhibiting the SMAD2-3 Pathway. Int J Mol Sci. 2020 Aug 4;21(15):5577. [Content Brief]
[2]. Morse A, et al. RAP-011 augments callus formation in closed fractures in rats. J Orthop Res. 2016 Feb;34(2):320-30. [Content Brief]
[3]. Langdon JM, et al. RAP-011, an activin receptor ligand trap, increases hemoglobin concentration in hepcidin transgenic mice. Am J Hematol. 2015 Jan;90(1):8-14. [Content Brief]
[4]. Agapova OA, et al. Ligand trap for the activin type IIA receptor protects against vascular disease and renal fibrosis in mice with chronic kidney disease. Kidney Int. 2016 Jun;89(6):1231-43. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Sotatercept (mIgG2a) Related Classifications
HY-P99590A Related Classifications
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