2. GPCR/G Protein
  3. Endothelin Receptor
  4. PD-156707

PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist. PD-156707 binds to human ET-A and ET-B receptors with Ki values of 0.17 nM and 133.8 nM, respectively. PD-156707 shows reversal of established chronic hypoxic pulmonary hypertension in rats. PD-156707 can be used for the study of diseases associated with abnormal ET-A receptor activation, particularly pulmonary hypertension, stroke, and heart failure.

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PD-156707

PD-156707 Chemical Structure

CAS No. : 162412-70-6

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PD-156707 Related Antibodies

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Description

PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist. PD-156707 binds to human ET-A and ET-B receptors with Ki values of 0.17 nM and 133.8 nM, respectively. PD-156707 shows reversal of established chronic hypoxic pulmonary hypertension in rats. PD-156707 can be used for the study of diseases associated with abnormal ET-A receptor activation, particularly pulmonary hypertension, stroke, and heart failure[1][2].

IC50 & Target[1]

ETA

0.17 μM (Ki)

ETB

133.8 μM (Ki)

In Vitro

PD-156707 inhibits inositol phosphate production induced by ET-1 in Ltk cells (IC50 = 2.4 nM) and arachidonic acid release stimulated by ET-1 in rabbit renal artery VSMC cells (IC50 = 1.1 nM)[1].
PD-156707 (0.1-10 μM) cause a rightward shift in the concentration-response curve of ET-1-stimulated contraction of rabbit femoral artery[1].
PD-156707 (1 μM) exerts a significant inhibitory effect on spontaneous neointimal proliferation of transverse sections of human saphenous vein[1].

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

PD-156707 Related Antibodies
In Vivo

PD-156707 (10-40 mg/kg, p.o., daily) shows dose-related reversal of established chronic hypoxic pulmonary hypertension and attenuation of right ventricular hypertrophy in rats[1].
PD-156707 (0.003-0.3 mg/kg/h, i.v. infusion, 1 h) shows dose-dependent inhibition of ET-1-induced renal vascular resistance (RVR) increase in rabbits[2].

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

Animal Model: Male New Zealand White rabbits (2-3 kg)[2]
Dosage: 0.003, 0.01, 0.03, 0.3 mg/kg/h
Administration: i.v. infusion, 1 h
Result: Showed dose-dependent inhibition of endothelin-1 (ET-1)-induced renal vascular resistance (RVR) increase.
Exerts no significant effect on baseline MAP, heart rate, RBF, or RVR.
Blocks ET-1-induced RVR increase without attenuating ET-1-induced MAP reduction.
Molecular Weight

528.48

Formula

C28H25NaO9
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(/C(C1=CC=C2OCOC2=C1)=C(C(C3=CC=C(C=C3)OC)=O)/CC4=CC(OC)=C(C(OC)=C4)OC)O[Na]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

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

Purity & Documentation
References
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PD-156707 Related Classifications

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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.

Keywords:

PD-156707162412-70-6PD156707PD 156707Endothelin ReceptorET-1ETA receptorvasoconstrictorInhibitorinhibitorinhibit

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