1. GPCR/G Protein Metabolic Enzyme/Protease
  2. Angiotensin Receptor Neprilysin
  3. TD-0212

TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (TD-0212 TFA) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

TD-0212 Chemical Structure

TD-0212 Chemical Structure

CAS No. : 1073549-10-6

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Description

TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP[1].

IC50 & Target

pKi: 8.9 (AT1)
pIC50: 9.2 (NEP)[1].

In Vitro

TD-0212 (compound 35) provides the enhanced activity of dual AT1/NEP inhibition with a potentially lower risk of angioedema relative to dual ACE/NEP inhibition[1].

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

In Vivo

TD-0212 (compound 35) produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and –independent hypertension[1].

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

Molecular Weight

527.65

Formula

C28H34FN3O4S

CAS No.
SMILES

OC(C1=CC=CC=C1C2=CC=C(CN3C(CNC([C@H](CC(C)C)S)=O)=C(CC)N=C3OCC)C(F)=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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TD-0212
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HY-114412
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