Canvuparatide
Based on 1 Customer Validation
Canvuparatide (MBX 2109) is a PTH analog prodrug that releases the biologically active peptide through temperature- and pH-controlled intramolecular cyclization. The peptide released by Canvuparatide binds to and activates the PTH1 receptor, stimulating dose-dependent cAMP accumulation. Canvuparatide can be used in research on hypoparathyroidism.
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- Pureté : 97.26%
- CAS No.: 2925554-87-4
- Formule: C263H441N65O81S2
- Masse moléculaire:5873.83
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
PTH1R |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
Canvuparatide (7.5-15 nmol/kg; s.c.; daily; 28 days) restores serum calcium and phosphate to normal levels and increases bone formation rate (BFR/BS) in PTX rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley rats[1]
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Dosage:4-12 nmol/kg
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Administration:s.c.; once daily; 28 days
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Result:No appreciable changes in body weight or food intake were observed after 28 days of daily SC dosing at 4, 8, and 12 nmol/kg.
Increased serum calcium less than 0.5 nmol/μL, with no dose response over the course of the study.
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Animal Model:Sprague Dawley rats (female, parathyroidectomized, low-calcium diet)[1]
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Dosage:10-40 nmol/kg (4 doses); 10-40 nmol/kg (10 days); 5-15 nmol/kg (10 days); 7.5-15 nmol/kg (28 days)
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Administration:s.c.; daily; 4 or 10 or 28 days
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Result:Exhibited a dose-proportional increase in serum calcium after 48 h at 10, 25, and 40 nmol/kg; the calcium level in the 40-nmol/kg group slightly exceeded that in sham rats, and this relationship was maintained 72 h after the last dose.
Increased serum calcium dose-proportionally but exceeded sham levels at the higher doses after daily dosing for up to 10 days; on days 7, 10, and 11 significant differences were observed between vehicle and sham controls, the 25-nmol/kg group, and the 40-nmol/kg group, and between vehicle and the 10-nmol/kg group on days 7 and 11.
A dose-proportional increase in serum calcium occurred at 3 days and continued through the end of study at 5, 10, and 15 nmol/kg, at which time calcium in sham rats was statistically identical to the high-dose-treated PTX rats.
Restored circulating calcium levels similar to sham animals by day 14 and maintained through day 28 at 7.5 and 15 nmol/kg/day.
Decreased serum phosphate dose-proportionally at 10, 25, and 40 nmol/kg for up to 10 days, most evident on day 7 and day 10; significant differences were observed between vehicle and sham controls and the 40-nmol/kg group on days 3 and 11.
Reduced circulating phosphate closer to the upper limit of normal, similar to sham controls over 28 days at 7.5 and 15 nmol/kg/day.
No statistically significant changes in serum P1NP were observed after 4 and 28 days.
Resulted in a numerical reduction of trabecular BV/TV versus untreated PTX rats (not significant) at each dose.
Had significantly less cortical bone area compared with PTX vehicle controls at 15 nmol/kg, with a similar trend at 7.5 nmol/kg.
Had significantly higher BFR/BS than vehicle-treated PTX rats at 15 nmol/kg, and MAR, MS/BS, and BFR/BS did not differ from sham controls; the 7.5 nmol/kg dose had no significant effect on BFR/BS.
Oc.S/BS was significantly higher in PTX rats treated with canvuparatide 15 nmol/kg compared with sham rats.
Led to significantly lower displacement to failure and total work to failure versus PTX vehicle controls, and lower total work to failure versus sham controls at 15 nmol/kg, whereas 7.5 nmol/kg had no significant effect.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2925554-87-4
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Appearance Solid
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Masse moléculaire 5873.83
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Formule C263H441N65O81S2
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Color White to off-white
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Synonyms
MBX 2109
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Sequence
DLys(γ-Glu-PEG2-PEG2-17-carboxyheptadecanoyl)-Sar-Ser-Val-Ser-Glu-Ile-Gln-Leu-Met-His-Asn-Leu-Gly-Lys-His-Leu-Asn-Ser-Met-Glu-Arg-Val-Glu-Trp-Leu-Arg-Lys-Lys-Leu-Gln-Asp-Val-His-Lys(γ-Glu-PEG2-PEG2-17-carboxyheptadecanoyl)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (17.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
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Fiche technique (283 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.1702 mL | 0.8512 mL | 1.7025 mL | 4.2562 mL |
| 5 mM | 0.0340 mL | 0.1702 mL | 0.3405 mL | 0.8512 mL | |
| 10 mM | 0.0170 mL | 0.0851 mL | 0.1702 mL | 0.4256 mL | |
| 15 mM | 0.0113 mL | 0.0567 mL | 0.1135 mL | 0.2837 mL |
Canvuparatide Related Classifications
HY-P10909 Related Classifications
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Keywords
- Canvuparatide
- 2925554-87-4
- MBX 2109
- MBX2109
- MBX-2109
- PTHR
- Drug Intermediate
- Parathyroid hormone receptor
- Drug Iintermediate
- PTH1 receptor
- serum calcium
- PTX rats
- endogenous PTH(1-84)
- hypoparathyroidism
- cAMP accumulation
- urinary calcium excretion
- PTH1 receptor agonist
- PTH analog prodrug
- bone formation rate
- Inhibitor
- inhibitor
- inhibit