Ingredient Details :Gibb-3-ene-1,10-dicarboxylic acid, 2,4a,7-trihydroxy-1-methyl-8-methylene-, 1,4a-lactone, (1alpha,2beta,4aalpha,4bbeta,10beta)-


TCMI-ID: TCMI05825


Physicochemical Property
Ingredient Name Gibb-3-ene-1,10-dicarboxylic acid, 2,4a,7-trihydroxy-1-methyl-8-methylene-, 1,4a-lactone, (1alpha,2beta,4aalpha,4bbeta,10beta)-
Pubchem CID 439551
Iupac name (1R,2R,5S,8S,9S,10R,12S)-5,12-dihydroxy-11-methyl-6-methylidene-16-oxo-15-oxapentacyclo[9.3.2.15,8.01,10.02,8]heptadec-13-ene-9-carboxylic acid
Molecular Formula C19H22O6
Molecular Weight 346.4
Isomeric smiles CC12[C@H](C=C[C@@]3([C@@H]1[C@@H]([C@]45[C@H]3CC[C@](C4)(C(=C)C5)O)C(=O)O)OC2=O)O
InChI InChI=1S/C19H22O6/c1-9-7-17-8-18(9,24)5-3-10(17)19-6-4-11(20)16(2,15(23)25-19)13(19)12(17)14(21)22/h4,6,10-13,20,24H,1,3,5,7-8H2,2H3,(H,21,22)/t10-,11+,12-,13-,16?,17+,18+,19-/m1/s1
InChIKey IXORZMNAPKEEDV-QTWFBFKQSA-N
External Database Links HERB2.0: HBIN027612   DrugBank: DB07814  
Structural Information
nHA(Number of hydrogen bond acceptors) 6
nHD(Number of hydrogen bond donors) 3
nRot(Number of rotatable bonds) 1
nRing(Number of rings) 5
MaxRing(Number of atoms in the biggest ring) 7
nHet(Number of heteroatoms) 6

Stability
nRig(Number of rigid bonds) 24
Flexibility 0.042
Stereo Centers(Number of stereocenters) 8

Solubility
TPSA(Topological polar surface area) 104.06
logS(The logarithm of aqueous solubility value) -3.079
logP(The logarithm of the n-octanol/water distribution coefficient) 0.556
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) -0.253

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.484
Synthetic accessibility score 6.69
Natural Product-likeness score 3.652
Lipinski Rule Accepted
GSK Rule Accepted
Golden Triangle Accepted

Absorption
Caco-2 Permeability -5.955
MDCK Permeability 2.54E-05
Pgp-substrate 0.917
HIA(human intestinal absorption) 0.052
F20%(20% Oral Bioavailability) 0.657
F30%(30% Oral Bioavailability) 0.262

Distribution
PPB(Plasma protein binding) 28.71%
VD(Volume Distribution) 0.395
BBB Penetration(Blood brain barrier penetration) 0.219
B3 Penetration(Blood brain barrier penetration) Non-Permeable
Fu(The fraction unbound in plasms) 59.71%

Metabolism
CYP1A2 inhibitor 0.002
CYP1A2 substrate 0.933
CYP2C19 inhibitor 0.009
CYP2C19 substrate 0.237
CYP2C9 inhibitor 0.004
CYP2C9 substrate 0.062
CYP2D6 inhibitor 0.004
CYP2D6 substrate 0.098
CYP3A4 inhibitor 0.258
CYP3A4 substrate 0.039

Excretion
CL(The clearance of a drug) 2.075
T1/2 0.397

Toxicology
NonBiodegradable Rule 0
Pfizer Rule Accepted
SR-MMP 0.423

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.947
IGC50 2.152
LC50FM 3.496
LC50DM 6.475

Reproductive Effects
NR-AR(Androgen receptor) 0.26
NR-AR-LBD(Androgen receptor) 0.928
NR-Aromatase 0.808
NR-ER(Estrogen receptor) 0.612
NR-ER-LBD(Estrogen receptor) 0.016

Allergy
Skin Sensitization Rule 1
Skin Sensitization 0.211

Acute Toxicity
Acute Toxicity Rule 3
Rat Oral Acute Toxicity 0.435

Organ Toxicity
hERG Blockers 0.135
H-HT(The human hepatotoxicity) 0.887
DILI(Drug-induced liver injury) 0.048

Primary Irritation
Eye Corrosion 0.004
Eye Irritation 0.015
Respiratory Toxicity 0.98

Mutagenic Effects
AMES Toxicity 0.029

Tumorigenic Effects
Carcinogencity 0.345
SR-ARE(Antioxidant Response Element) 0.714
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.888
SR-p53 0.974

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