CGS 35066

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Cat.No. 2512 - CGS 35066 | C16H16NO6P | CAS No. 261619-50-5
Description: Endothelin-converting enzyme (ECE) inhibitor
Chemical Name: α-[(S)-(Phosphonomethyl)amino]-3-dibenzofuranpropanoic acid
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews (1)
Literature (1)

Biological Activity

Potent endothelin-converting enzyme (ECE) inhibitor that displays > 100-fold selectivity over neutral endopeptidase 24.11 (IC50 values are 22 and 2300 nM respectively). Blocks the hypertensive effects induced by big ET-1 in vitro and reduces the magnitude of cerebral vasospasm following subarachnoid hemorrhage (SAH).

Technical Data

M. Wt 349.28
Formula C16H16NO6P
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 261619-50-5
PubChem ID 9863167
InChI Key CRUVAUSVWLATAE-ZDUSSCGKSA-N
Smiles O=C([C@@H](NCP(O)(O)=O)CC1=CC3=C(C2=CC=CC=C2O3)C=C1)O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. NaOH 34.92 100

Preparing Stock Solutions

The following data is based on the product molecular weight 349.28. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.86 mL 14.32 mL 28.63 mL
5 mM 0.57 mL 2.86 mL 5.73 mL
10 mM 0.29 mL 1.43 mL 2.86 mL
50 mM 0.06 mL 0.29 mL 0.57 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

De Lombaert et al (2000) Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action. J.Med.Chem. 43 488 PMID: 10669576

Trapani et al (2000) Pharmacological properties of CGS 35066, a potent and selective endothelin-converting enzyme inhibitor, in conscious rats. J.Cardiovasc.Pharmacol. 36 S40 PMID: 11078331

Kwan et al (2002) Attenuation of SAH-induced cerebral vasospasm by a selective ECE inhibitor. Neuropharmacol.Neurotoxicol. 13 197


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Keywords: CGS 35066, CGS 35066 supplier, Endothelin-converting, enzyme, ECE, inhibitors, inhibits, Proteases, Proteinases, CGS35066, Other, 2512, Tocris Bioscience

Citations for CGS 35066

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Reviews for CGS 35066

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Piglet Unilateral Ureteral Obstruction model to study kidney injury and role of RAAS pathway..
By Vaishali Soni on 01/18/2018
Assay Type: In Vivo
Species: Other

Piglet Unilateral Ureteral Obstruction model to study kidney injury and role of RAAS pathway.Sample used for NGAL measurement (ELISA) is Urine.Bosentan: dual endothelin receptor antagonistCGS 35066: endothelin-converting enzyme (ECE) inhibitorPyr3:Selective antagonist of the canonical transient receptor potential channel 3 (TRPC3)All compound used intravenously after performing surgery on piglet.

Compound was dissolved in DMSO to make stock and then formulated using 20% captisol in normal saline. However, we can not disclose the dose used to perform study due to confidentiality of data that not yet published.

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