Ingredient Details :(1S,4Z,12S,13R)-5,10-dimethyl-8,14,16-trioxatetracyclo[10.2.2.01,13.07,11]hexadeca-4,7(11),9-trien-15-one


TCMI-ID: TCMI22392


Physicochemical Property
Ingredient Name (1S,4Z,12S,13R)-5,10-dimethyl-8,14,16-trioxatetracyclo[10.2.2.01,13.07,11]hexadeca-4,7(11),9-trien-15-one
Pubchem CID 127258921
Iupac name (1S,4Z,12S,13R)-5,10-dimethyl-8,14,16-trioxatetracyclo[10.2.2.01,13.07,11]hexadeca-4,7(11),9-trien-15-one
Molecular Formula C15H16O4
Molecular Weight 260.28
Isomeric smiles C/C/1=C/CC[C@@]23[C@H](O2)[C@H](C4=C(C1)OC=C4C)OC3=O
InChI InChI=1S/C15H16O4/c1-8-4-3-5-15-13(19-15)12(18-14(15)16)11-9(2)7-17-10(11)6-8/h4,7,12-13H,3,5-6H2,1-2H3/b8-4-/t12-,13+,15-/m0/s1
InChIKey KBMSVODXFLAQNJ-ILKNJTSDSA-N
External Database Links
Structural Information
nHA(Number of hydrogen bond acceptors) 4
nHD(Number of hydrogen bond donors) 0
nRot(Number of rotatable bonds) 0
nRing(Number of rings) 4
MaxRing(Number of atoms in the biggest ring) 14
nHet(Number of heteroatoms) 4

Stability
nRig(Number of rigid bonds) 20
Flexibility 0
Stereo Centers(Number of stereocenters) 3

Solubility
TPSA(Topological polar surface area) 51.97
logS(The logarithm of aqueous solubility value) -4.154
logP(The logarithm of the n-octanol/water distribution coefficient) 2.53
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) 2.695

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.409
Synthetic accessibility score 5.798
Natural Product-likeness score 3.448
Lipinski Rule Accepted
GSK Rule Accepted
Golden Triangle Accepted

Absorption
Caco-2 Permeability -4.674
MDCK Permeability 1.82E-05
Pgp-substrate 0.09
HIA(human intestinal absorption) 0.016
F20%(20% Oral Bioavailability) 0.01
F30%(30% Oral Bioavailability) 0.425

Distribution
PPB(Plasma protein binding) 89.64%
VD(Volume Distribution) 2.835
BBB Penetration(Blood brain barrier penetration) 0.61
B3 Penetration(Blood brain barrier penetration) Permeable
Fu(The fraction unbound in plasms) 7.35%

Metabolism
CYP1A2 inhibitor 0.059
CYP1A2 substrate 0.746
CYP2C19 inhibitor 0.553
CYP2C19 substrate 0.764
CYP2C9 inhibitor 0.162
CYP2C9 substrate 0.085
CYP2D6 inhibitor 0.024
CYP2D6 substrate 0.725
CYP3A4 inhibitor 0.62
CYP3A4 substrate 0.421

Excretion
CL(The clearance of a drug) 14.826
T1/2 0.552

Toxicology
NonBiodegradable Rule 2
Pfizer Rule Accepted
SR-MMP 0.337

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.036
IGC50 4.736
LC50FM 6.251
LC50DM 6.724

Reproductive Effects
NR-AR(Androgen receptor) 0.009
NR-AR-LBD(Androgen receptor) 0.368
NR-Aromatase 0.77
NR-ER(Estrogen receptor) 0.534
NR-ER-LBD(Estrogen receptor) 0.494

Allergy
Skin Sensitization Rule 4
Skin Sensitization 0.592

Acute Toxicity
Acute Toxicity Rule 4
Rat Oral Acute Toxicity 0.888

Organ Toxicity
hERG Blockers 0.034
H-HT(The human hepatotoxicity) 0.757
DILI(Drug-induced liver injury) 0.826

Primary Irritation
Eye Corrosion 0.016
Eye Irritation 0.025
Respiratory Toxicity 0.959

Mutagenic Effects
AMES Toxicity 0.636

Tumorigenic Effects
Carcinogencity 0.86
SR-ARE(Antioxidant Response Element) 0.589
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.118
SR-p53 0.941

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