Mergetpa
Based on 1 Customer Validation
Mergetpa is a reversible Arg-carboxypeptidase inhibitor with high affinity. Mergetpa reduces B1R. Mergetpa blocks the overexpression of IL-1β protein and mRNA in glucose-fed rats. Mergetpa significantly increases the expression of IL-1β protein in the renal cortex. Mergetpa is used to block the conversion of kinins and B2 receptor antagonists into metabolites lacking the C-terminal arginine. Mergetpa inhibits the time-dependent enhancement of the response of isolated rabbit aorta to bradykinin. Mergetpa preserves the chemotactic activity of full-length SDF-1α on cells. Mergetpa reverses hyperglycemia, excessive weight gain, elevated levels of oxidative stress markers and overexpression of inflammatory markers in glucose-fed rats.
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- Pureté: 95.55%
- CAS No.: 77102-28-4
- Formule: C7H15N3O2S2
- Masse moléculaire:237.34
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Stockage:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, 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
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Voir tous les produits spécifiques à Isoform Bradykinin Receptor
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Activité biologique
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IL-1β |
Bradykinin B1 Receptor (B1R) |
In isolated rabbit aortas, mergetpa (8.43×10-6 M; 1-6 h) prevents the time-dependent increase in bradykinin-induced contraction, reduces the apparent affinity of B2 receptor antagonists, and does not reduce the apparent affinity of a B1 receptor antagonist[1].
In isolated rabbit jugular veins, mergetpa (8.42×10-6 M) does not alter the apparent affinity of B2 receptor antagonists[1].
Mergetpa (5 μM; 10 min) preserves the chemotactic activity of SDF-1α (1-68) for bone marrow and cord blood CD34+ cells[3].
Mergetpa (5 μM; 30 min) increases the chemotactic response of THP-1 cells to full-length SDF-1α (1-68) by a factor of 1.4, with no effect on migration toward truncated des-lys SDF-1α (1-67)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 24-30 days old, 50-75 g at study initiation, insulin resistance induced via 9 weeks of ad libitum 10% D-glucose drinking solution)[2]
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Dosage:1 mg/kg
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Administration:s.c.; twice daily; 7 days
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Result:Normalized two-fold elevated blood glucose levels in glucose-fed rats to values not significantly different from control rats.
Halved four-fold elevated plasma insulin levels in glucose-fed rats (reduction did not reach statistical significance).
Markedly reduced (P < 0.05) elevated HOMA index of insulin resistance in glucose-fed rats, though not to full control levels.
Induced significant body weight loss (18 g, P < 0.05) in glucose-fed rats, reversing their previously increased body weight gain, but did not affect body weight gain in control rats.
Did not alter elevated plasma leptin levels or systolic blood pressure in glucose-fed rats.
Normalized elevated basal superoxide anion production in the aorta of glucose-fed rats to control levels.
Significantly reduced (P < 0.05) enhanced nitrotyrosine expression in the renal cortex and aorta of glucose-fed rats to levels not significantly different from control rats.
Restored significantly enhanced B1R protein and mRNA expression in the renal cortex, thoracic aorta, and liver of glucose-fed rats to control levels.
Completely blocked (P < 0.05) enhanced CPM protein expression in the renal cortex, thoracic aorta, and liver of glucose-fed rats.
Abolished significantly enhanced iNOS protein expression in the renal cortex, thoracic aorta, and liver of glucose-fed rats.
Fully blocked (P < 0.05) enhanced IL-1β protein and mRNA expression in the renal cortex, thoracic aorta, and liver of glucose-fed rats.
Did not significantly affect blood glucose, plasma insulin, HOMA index, superoxide anion production, B1R expression, CPM expression, or iNOS expression in control rats; significantly reduced nitrotyrosine expression in control aorta (but not renal cortex) and increased IL-1β protein expression in control renal cortex.
Chemical Information
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CAS No. 77102-28-4
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Appearance Solid
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Masse moléculaire 237.34
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Formule C7H15N3O2S2
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Color White to off-white
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SMILES
O=C(C(CSCCNC(N)=N)CS)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Solvant et solubilité
H2O : 15 mg/mL (63.20 mM; Need ultrasonic)
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 (stored under nitrogen, 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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (stored under nitrogen, 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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (275 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Regoli D, et al. Conversion of kinins and their antagonists into B1 receptor activators and blockers in isolated vessels. Eur J Pharmacol. 1986;127(3):219-224. [Content Brief]
[2]. Haddad Y, et al. Kininase 1 As a Preclinical Therapeutic Target for Kinin B1 Receptor in Insulin Resistance. Front Pharmacol. 2017;8:509. Published 2017 Aug 2. [Content Brief]
[3]. Marquez-Curtis L, et al. Carboxypeptidase M expressed by human bone marrow cells cleaves the C-terminal lysine of stromal cell-derived factor-1alpha: another player in hematopoietic stem/progenitor cell mobilization? Stem Cells. 2008 May;26(5):1211-20. [Content Brief]
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 (stored under nitrogen, 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 4.2134 mL | 21.0668 mL | 42.1336 mL | 105.3341 mL |
| 5 mM | 0.8427 mL | 4.2134 mL | 8.4267 mL | 21.0668 mL | |
| 10 mM | 0.4213 mL | 2.1067 mL | 4.2134 mL | 10.5334 mL | |
| 15 mM | 0.2809 mL | 1.4045 mL | 2.8089 mL | 7.0223 mL | |
| 20 mM | 0.2107 mL | 1.0533 mL | 2.1067 mL | 5.2667 mL | |
| 25 mM | 0.1685 mL | 0.8427 mL | 1.6853 mL | 4.2134 mL | |
| 30 mM | 0.1404 mL | 0.7022 mL | 1.4045 mL | 3.5111 mL | |
| 40 mM | 0.1053 mL | 0.5267 mL | 1.0533 mL | 2.6334 mL | |
| 50 mM | 0.0843 mL | 0.4213 mL | 0.8427 mL | 2.1067 mL | |
| 60 mM | 0.0702 mL | 0.3511 mL | 0.7022 mL | 1.7556 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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