Ingredient Details :(2R)-2-[(3S,10S,13R,14R,16R,17R)-3,16-dihydroxy-4,4,10,13,14-pentamethyl-2,3,5,6,12,15,16,17-octahydro-1H-cyclopenta[a]phenanthren-17-yl]-6-methyl-5-methylideneheptanoic acid


TCMI-ID: TCMI05259


Physicochemical Property
Ingredient Name (2R)-2-[(3S,10S,13R,14R,16R,17R)-3,16-dihydroxy-4,4,10,13,14-pentamethyl-2,3,5,6,12,15,16,17-octahydro-1H-cyclopenta[a]phenanthren-17-yl]-6-methyl-5-methylideneheptanoic acid
Pubchem CID 216251
Iupac name (2R)-2-[(3S,10S,13R,14R,16R,17R)-3,16-dihydroxy-4,4,10,13,14-pentamethyl-2,3,5,6,12,15,16,17-octahydro-1H-cyclopenta[a]phenanthren-17-yl]-6-methyl-5-methylideneheptanoic acid
Molecular Formula C31H48O4
Molecular Weight 484.7
Isomeric smiles CC(C)C(=C)CC[C@H]([C@H]1[C@@H](C[C@@]2([C@@]1(CC=C3C2=CCC4[C@@]3(CC[C@@H](C4(C)C)O)C)C)C)O)C(=O)O
InChI InChI=1S/C31H48O4/c1-18(2)19(3)9-10-20(27(34)35)26-23(32)17-31(8)22-11-12-24-28(4,5)25(33)14-15-29(24,6)21(22)13-16-30(26,31)7/h11,13,18,20,23-26,32-33H,3,9-10,12,14-17H2,1-2,4-8H3,(H,34,35)/t20-,23-,24?,25+,26+,29-,30-,31+/m1/s1
InChIKey LADJWZMBZBVBSB-DWSVKRSBSA-N
External Database Links
Structural Information
nHA(Number of hydrogen bond acceptors) 4
nHD(Number of hydrogen bond donors) 3
nRot(Number of rotatable bonds) 6
nRing(Number of rings) 4
MaxRing(Number of atoms in the biggest ring) 17
nHet(Number of heteroatoms) 4

Stability
nRig(Number of rigid bonds) 22
Flexibility 0.273
Stereo Centers(Number of stereocenters) 8

Solubility
TPSA(Topological polar surface area) 77.76
logS(The logarithm of aqueous solubility value) -4.799
logP(The logarithm of the n-octanol/water distribution coefficient) 5.422
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) 4.355

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.374
Synthetic accessibility score 5.14
Natural Product-likeness score 3.527
Lipinski Rule Accepted
GSK Rule Rejected
Golden Triangle Accepted

Absorption
Caco-2 Permeability -5.057
MDCK Permeability 2.29E-05
Pgp-substrate 0.003
HIA(human intestinal absorption) 0.004
F20%(20% Oral Bioavailability) 0.044
F30%(30% Oral Bioavailability) 0.025

Distribution
PPB(Plasma protein binding) 93.87%
VD(Volume Distribution) 0.748
BBB Penetration(Blood brain barrier penetration) 0.084
B3 Penetration(Blood brain barrier penetration) Permeable
Fu(The fraction unbound in plasms) 4.11%

Metabolism
CYP1A2 inhibitor 0.007
CYP1A2 substrate 0.153
CYP2C19 inhibitor 0.011
CYP2C19 substrate 0.912
CYP2C9 inhibitor 0.105
CYP2C9 substrate 0.916
CYP2D6 inhibitor 0.002
CYP2D6 substrate 0.28
CYP3A4 inhibitor 0.078
CYP3A4 substrate 0.287

Excretion
CL(The clearance of a drug) 2.69
T1/2 0.203

Toxicology
NonBiodegradable Rule 0
Pfizer Rule Accepted
SR-MMP 0.798

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.944
IGC50 3.801
LC50FM 4.825
LC50DM 4.939

Reproductive Effects
NR-AR(Androgen receptor) 0.489
NR-AR-LBD(Androgen receptor) 0.096
NR-Aromatase 0.787
NR-ER(Estrogen receptor) 0.122
NR-ER-LBD(Estrogen receptor) 0.017

Allergy
Skin Sensitization Rule 0
Skin Sensitization 0.871

Acute Toxicity
Acute Toxicity Rule 1
Rat Oral Acute Toxicity 0.317

Organ Toxicity
hERG Blockers 0.057
H-HT(The human hepatotoxicity) 0.558
DILI(Drug-induced liver injury) 0.01

Primary Irritation
Eye Corrosion 0.006
Eye Irritation 0.016
Respiratory Toxicity 0.972

Mutagenic Effects
AMES Toxicity 0.01

Tumorigenic Effects
Carcinogencity 0.552
SR-ARE(Antioxidant Response Element) 0.15
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.059
SR-p53 0.689

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