2. Metabolic Enzyme/Protease GPCR/G Protein Immunology/Inflammation
  3. Carboxypeptidase Bradykinin Receptor Interleukin Related
  4. Mergetpa

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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Mergetpa

Mergetpa Chemical Structure

CAS No. : 77102-28-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Mergetpa Related Antibodies

Top Publications Citing Use of Products

View All Bradykinin Receptor Isoform Specific Products:

View All Isoforms
Bradykinin B1 Receptor (B1R) Bradykinin B2 Receptor (B2R)

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

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[1][2][3].

IC50 & Target[1]

IL-1β

 

Bradykinin B1 Receptor (B1R)

 

In Vitro

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.

Mergetpa Related Antibodies
In Vivo

Mergetpa (1 mg/kg; s.c.; twice daily; 7 days) normalizes hyperglycemia, reverses body weight gain, restores oxidative stress markers to control levels, and blocks enhanced expression of inflammatory and B1R pathway markers in glucose-fed rats with insulin resistance, though it does not affect hyperleptinemia or hypertension[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 1 mg/kg
Administration: s.c.; twice daily; 7 days
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.
Molecular Weight

237.34

Formula

C7H15N3O2S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(CSCCNC(N)=N)CS)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 15 mg/mL (63.20 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2134 mL 21.0668 mL 42.1336 mL
5 mM 0.8427 mL 4.2134 mL 8.4267 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.
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Working solution concentration: mg/mL
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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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Mergetpa Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mergetpa77102-28-4CarboxypeptidaseBradykinin ReceptorInterleukin RelatedILSDF-1αcarboxypeptidase MTHP-1 cellscarboxypeptidase Nbradykininhuman carboxypeptidase Mhematopoietic stem/progenitor cellsinsulin resistanceB2 receptorrabbit isolated aortaeInhibitorinhibitorinhibit

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