| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C7H15N3O2S2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Mergetpa is a reversible, high-affinity inhibitor of Arg-carboxypeptidase that reduces B1R and blocks the overexpression of IL-1β protein and mRNA in glucose-fed rats, while significantly increasing IL-1β protein expression in the renal cortex. It blocks the conversion of kinins and B2 receptor antagonists into metabolites lacking the C-terminal arginine, inhibits the time-dependent enhancement of isolated rabbit aorta's response to bradykinin, and preserves the chemotactic activity of full-length SDF-1α on cells. It also reverses hyperglycemia, excessive weight gain, elevated oxidative stress markers, and overexpression of inflammatory markers in glucose-fed rats[1][2][3]. It is supplied as a white to off-white solid (C7H15N3O2S2, MW 237.34) at 95.55% purity.
Physical & Chemical Properties
| CAS Number | 77102-28-4 |
|---|---|
| Molecular Formula | C7H15N3O2S2 |
| Molecular Weight | 237.34 g/mol |
| Purity | 95.55% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(C(CSCCNC(N)=N)CS)O |
| Target | IL-1β, Bradykinin B1 Receptor (B1R) |
| Signaling Pathway | Metabolic Enzyme/Protease; GPCR/G Protein; Immunology/Inflammation |
| Solubility | In Vitro: H2O: 15 mg/mL (63.20 mM; Requires sonication) |
| 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). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| H2O | 15 mg/mL (63.20 mM) | requires sonication |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); stored under nitrogen, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
Data provided by the manufacturer.
In Vitro
In isolated rabbit aortas, mergetpa (8.43×10-6 M; 1-6 h) blocks the time-dependent increase in bradykinin-induced contraction and lowers the apparent affinity of B2 receptor antagonists, but does not lower the apparent affinity of a B1 receptor antagonist[1]. In jugular veins isolated from rabbits, mergetpa (8.42×10-6 M) leaves the apparent affinity of B2 receptor antagonists unchanged[1]. Mergetpa (5 μM; 10 min) maintains the chemotactic activity of SDF-1α (1-68) toward CD34+ cells from bone marrow and cord blood[3]. Mergetpa (5 μM; 30 min) boosts THP-1 cell chemotaxis toward full-length SDF-1α (1-68) by a factor of 1.4, while migration toward truncated des-lys SDF-1α (1-67) is unaffected[3].
In Vivo
In glucose-fed rats with insulin resistance, Mergetpa (1 mg/kg; s.c.; twice daily; 7 days) returns hyperglycemia to normal, reverses body weight gain, returns oxidative stress markers to control levels, and blocks the enhanced expression of inflammatory and B1R pathway markers, but it does not affect hyperleptinemia or hypertension[2].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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