Ingredient Details :3-O-(2'E,4'Z-decadienoyl)ingenol


TCMI-ID: TCMI18459


Physicochemical Property
Ingredient Name 3-O-(2'E,4'Z-decadienoyl)ingenol
Pubchem CID 44575953
Iupac name [(1S,4S,5S,6R,9S,10R,12R,14R)-5,6-dihydroxy-7-(hydroxymethyl)-3,11,11,14-tetramethyl-15-oxo-4-tetracyclo[7.5.1.01,5.010,12]pentadeca-2,7-dienyl] (2E,4Z)-deca-2,4-dienoate
Molecular Formula C30H42O6
Molecular Weight 498.6
Isomeric smiles CCCCC/C=C\C=C\C(=O)O[C@H]1C(=C[C@@]23[C@@]1([C@@H](C(=C[C@H](C2=O)[C@H]4[C@H](C4(C)C)C[C@H]3C)CO)O)O)C
InChI InChI=1S/C30H42O6/c1-6-7-8-9-10-11-12-13-23(32)36-27-18(2)16-29-19(3)14-22-24(28(22,4)5)21(26(29)34)15-20(17-31)25(33)30(27,29)35/h10-13,15-16,19,21-22,24-25,27,31,33,35H,6-9,14,17H2,1-5H3/b11-10-,13-12+/t19-,21+,22-,24+,25-,27+,29+,30+/m1/s1
InChIKey XMXZQPNIMGCMHC-JFSCPWEMSA-N
External Database Links ChEMBL: CHEMBL486883  
Structural Information
nHA(Number of hydrogen bond acceptors) 6
nHD(Number of hydrogen bond donors) 3
nRot(Number of rotatable bonds) 9
nRing(Number of rings) 4
MaxRing(Number of atoms in the biggest ring) 14
nHet(Number of heteroatoms) 6

Stability
nRig(Number of rigid bonds) 22
Flexibility 0.409
Stereo Centers(Number of stereocenters) 8

Solubility
TPSA(Topological polar surface area) 104.06
logS(The logarithm of aqueous solubility value) -4.492
logP(The logarithm of the n-octanol/water distribution coefficient) 4.96
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) 4.193

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.153
Synthetic accessibility score 6.227
Natural Product-likeness score 3.271
Lipinski Rule Accepted
GSK Rule Rejected
Golden Triangle Accepted

Absorption
Caco-2 Permeability -4.608
MDCK Permeability 4.93E-05
Pgp-substrate 0.996
HIA(human intestinal absorption) 0.016
F20%(20% Oral Bioavailability) 0.954
F30%(30% Oral Bioavailability) 0.154

Distribution
PPB(Plasma protein binding) 95.53%
VD(Volume Distribution) 1.515
BBB Penetration(Blood brain barrier penetration) 0.15
B3 Penetration(Blood brain barrier penetration) Permeable
Fu(The fraction unbound in plasms) 2.06%

Metabolism
CYP1A2 inhibitor 0.111
CYP1A2 substrate 0.103
CYP2C19 inhibitor 0.348
CYP2C19 substrate 0.461
CYP2C9 inhibitor 0.833
CYP2C9 substrate 0.092
CYP2D6 inhibitor 0.17
CYP2D6 substrate 0.063
CYP3A4 inhibitor 0.93
CYP3A4 substrate 0.352

Excretion
CL(The clearance of a drug) 8.308
T1/2 0.102

Toxicology
NonBiodegradable Rule 1
Pfizer Rule Accepted
SR-MMP 0.91

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.974
IGC50 5.09
LC50FM 7.363
LC50DM 7.583

Reproductive Effects
NR-AR(Androgen receptor) 0.063
NR-AR-LBD(Androgen receptor) 0.01
NR-Aromatase 0.932
NR-ER(Estrogen receptor) 0.138
NR-ER-LBD(Estrogen receptor) 0.007

Allergy
Skin Sensitization Rule 6
Skin Sensitization 0.659

Acute Toxicity
Acute Toxicity Rule 5
Rat Oral Acute Toxicity 0.944

Organ Toxicity
hERG Blockers 0.012
H-HT(The human hepatotoxicity) 0.604
DILI(Drug-induced liver injury) 0.941

Primary Irritation
Eye Corrosion 0.174
Eye Irritation 0.316
Respiratory Toxicity 0.984

Mutagenic Effects
AMES Toxicity 0.04

Tumorigenic Effects
Carcinogencity 0.075
SR-ARE(Antioxidant Response Element) 0.731
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.291
SR-p53 0.91

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