An IP receptor agonist
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Ralinepag

Item No. 30009

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[trans-4-[[[[(4-chlorophenyl)phenylamino]carbonyl]oxy]methyl]cyclohexyl]methoxy]-acetic acid
CAS Number
1187856-49-0
Molecular Formula
C23H26ClNO5
Formula Weight
431.9
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 15mg/mLDMF:PBS (pH 7.2) (1:8): 0.11mg/mLDMSO: 10mg/mLEthanol: 10mg/mL
SMILES
O=C(OC[C@@H]1CC[C@@H](COCC(O)=O)CC1)N(C2=CC=C(Cl)C=C2)C3=CC=CC=C3
InChi Code
InChI=1S/C23H26ClNO5/c24-19-10-12-21(13-11-19)25(20-4-2-1-3-5-20)23(28)30-15-18-8-6-17(7-9-18)14-29-16-22(26)27/h1-5,10-13,17-18H,6-9,14-16H2,(H,26,27)/t17-,18-
InChi Key
NPDKXVKJRHPDQT-IYARVYRRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $148

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    10 mg

    $255

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    25 mg

    $341

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    Product Description

    Ralinepag is a prostaglandin I2 (PGI2) receptor (IP) agonist (Ki = 3 nM).1 It is selective for IP over the PGD2 receptor (DP1) and the PGE2 receptor subtypes EP1-4 (Kis = 2,600, 9,600, 611, 143, and 678 nM, respectively, in radioligand binding assays). Ralinepag induces cAMP accumulation in CHO-K1 cells expressing human recombinant IP (EC50 = 8.5 nM). In vivo, ralinepag (30 mg/kg) prevents increases in pulmonary arterial pressure and vessel wall thickness in a rat model of monocrotaline-induced pulmonary arterial hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tran, T.-A., Kramer, B., Shin, Y.-J., et al. Discovery of 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralingepag): An orally active prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension. J. Med. Chem. 60(3), 913-927 (2017).