Ingredient Details :2beta-(3,4-Dimethoxyphenyl)-3alpha-methyl-3aalpha-methoxy-5-allyl-2,3,3a,6-tetrahydrobenzofuran-6-one


TCMI-ID: TCMI13499


Physicochemical Property
Ingredient Name 2beta-(3,4-Dimethoxyphenyl)-3alpha-methyl-3aalpha-methoxy-5-allyl-2,3,3a,6-tetrahydrobenzofuran-6-one
Pubchem CID 10915273
Iupac name (2R,3S,3aS)-2-(3,4-dimethoxyphenyl)-3a-methoxy-3-methyl-5-prop-2-enyl-2,3-dihydro-1-benzofuran-6-one
Molecular Formula C21H24O5
Molecular Weight 356.4
Isomeric smiles C[C@H]1[C@@H](OC2=CC(=O)C(=C[C@]12OC)CC=C)C3=CC(=C(C=C3)OC)OC
InChI InChI=1S/C21H24O5/c1-6-7-15-12-21(25-5)13(2)20(26-19(21)11-16(15)22)14-8-9-17(23-3)18(10-14)24-4/h6,8-13,20H,1,7H2,2-5H3/t13-,20+,21-/m0/s1
InChIKey VDYACOATPFOZIO-DYXDTQHNSA-N
External Database Links HERB2.0: HBIN023341   TCMSID: 13353  
Structural Information
nHA(Number of hydrogen bond acceptors) 5
nHD(Number of hydrogen bond donors) 0
nRot(Number of rotatable bonds) 6
nRing(Number of rings) 3
MaxRing(Number of atoms in the biggest ring) 9
nHet(Number of heteroatoms) 5

Stability
nRig(Number of rigid bonds) 18
Flexibility 0.333
Stereo Centers(Number of stereocenters) 3

Solubility
TPSA(Topological polar surface area) 53.99
logS(The logarithm of aqueous solubility value) -4.536
logP(The logarithm of the n-octanol/water distribution coefficient) 3.193
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) 2.938

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.727
Synthetic accessibility score 4.064
Natural Product-likeness score 2.222
Lipinski Rule Accepted
GSK Rule Accepted
Golden Triangle Accepted

Absorption
Caco-2 Permeability -4.567
MDCK Permeability 1.48E-05
Pgp-substrate 0.001
HIA(human intestinal absorption) 0.015
F20%(20% Oral Bioavailability) 0.043
F30%(30% Oral Bioavailability) 0.716

Distribution
PPB(Plasma protein binding) 85.12%
VD(Volume Distribution) 1.144
BBB Penetration(Blood brain barrier penetration) 0.229
B3 Penetration(Blood brain barrier penetration) Permeable
Fu(The fraction unbound in plasms) 7.76%

Metabolism
CYP1A2 inhibitor 0.245
CYP1A2 substrate 0.956
CYP2C19 inhibitor 0.799
CYP2C19 substrate 0.835
CYP2C9 inhibitor 0.664
CYP2C9 substrate 0.236
CYP2D6 inhibitor 0.775
CYP2D6 substrate 0.383
CYP3A4 inhibitor 0.92
CYP3A4 substrate 0.865

Excretion
CL(The clearance of a drug) 9.131
T1/2 0.447

Toxicology
NonBiodegradable Rule 2
Pfizer Rule Rejected
SR-MMP 0.437

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.75
IGC50 3.99
LC50FM 6.072
LC50DM 5.998

Reproductive Effects
NR-AR(Androgen receptor) 0.831
NR-AR-LBD(Androgen receptor) 0.277
NR-Aromatase 0.79
NR-ER(Estrogen receptor) 0.414
NR-ER-LBD(Estrogen receptor) 0.061

Allergy
Skin Sensitization Rule 3
Skin Sensitization 0.852

Acute Toxicity
Acute Toxicity Rule 2
Rat Oral Acute Toxicity 0.447

Organ Toxicity
hERG Blockers 0.088
H-HT(The human hepatotoxicity) 0.605
DILI(Drug-induced liver injury) 0.174

Primary Irritation
Eye Corrosion 0.004
Eye Irritation 0.025
Respiratory Toxicity 0.974

Mutagenic Effects
AMES Toxicity 0.04

Tumorigenic Effects
Carcinogencity 0.913
SR-ARE(Antioxidant Response Element) 0.696
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.052
SR-p53 0.791

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