Ingredient Details :(1R,6R,7S,8S,9R,10S,11S,13S,16S,17R)-8-tert-butyl-6,9,17-trihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,18-trione


TCMI-ID: TCMI21716


Physicochemical Property
Ingredient Name (1R,6R,7S,8S,9R,10S,11S,13S,16S,17R)-8-tert-butyl-6,9,17-trihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,18-trione
Pubchem CID 102004438
Iupac name (1R,6R,7S,8S,9R,10S,11S,13S,16S,17R)-8-tert-butyl-6,9,17-trihydroxy-16-methyl-2,4,14,19-tetraoxahexacyclo[8.7.2.01,11.03,7.07,11.013,17]nonadecane-5,15,18-trione
Molecular Formula C20H24O10
Molecular Weight 424.4
Isomeric smiles C[C@@H]1C(=O)O[C@@H]2[C@]1([C@@]34C(=O)O[C@H]5[C@]3(C2)[C@@]6([C@@H]([C@H]5O)C(C)(C)C)[C@H](C(=O)OC6O4)O)O
InChI InChI=1S/C20H24O10/c1-6-12(23)27-7-5-17-11-8(21)9(16(2,3)4)18(17)10(22)13(24)29-15(18)30-20(17,14(25)28-11)19(6,7)26/h6-11,15,21-22,26H,5H2,1-4H3/t6-,7+,8-,9+,10+,11-,15?,17-,18+,19-,20-/m1/s1
InChIKey LMEHVEUFNRJAAV-GKDYGBOSSA-N
External Database Links
Structural Information
nHA(Number of hydrogen bond acceptors) 10
nHD(Number of hydrogen bond donors) 3
nRot(Number of rotatable bonds) 1
nRing(Number of rings) 6
MaxRing(Number of atoms in the biggest ring) 12
nHet(Number of heteroatoms) 10

Stability
nRig(Number of rigid bonds) 27
Flexibility 0.037
Stereo Centers(Number of stereocenters) 11

Solubility
TPSA(Topological polar surface area) 148.82
logS(The logarithm of aqueous solubility value) -4.645
logP(The logarithm of the n-octanol/water distribution coefficient) 1.427
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) 0.406

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.314
Synthetic accessibility score 6.283
Natural Product-likeness score 3.27
Lipinski Rule Accepted
GSK Rule Rejected
Golden Triangle Accepted

Absorption
Caco-2 Permeability -5.529
MDCK Permeability 0.000102813
Pgp-substrate 0.953
HIA(human intestinal absorption) 0.009
F20%(20% Oral Bioavailability) 0.028
F30%(30% Oral Bioavailability) 0.944

Distribution
PPB(Plasma protein binding) 43.86%
VD(Volume Distribution) 0.576
BBB Penetration(Blood brain barrier penetration) 0.186
B3 Penetration(Blood brain barrier penetration) Non-Permeable
Fu(The fraction unbound in plasms) 52.42%

Metabolism
CYP1A2 inhibitor 0.01
CYP1A2 substrate 0.101
CYP2C19 inhibitor 0.015
CYP2C19 substrate 0.401
CYP2C9 inhibitor 0.004
CYP2C9 substrate 0.029
CYP2D6 inhibitor 0.006
CYP2D6 substrate 0.126
CYP3A4 inhibitor 0.041
CYP3A4 substrate 0.109

Excretion
CL(The clearance of a drug) 2.206
T1/2 0.113

Toxicology
NonBiodegradable Rule 2
Pfizer Rule Accepted
SR-MMP 0.787

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.682
IGC50 3.881
LC50FM 4.74
LC50DM 7.57

Reproductive Effects
NR-AR(Androgen receptor) 0.992
NR-AR-LBD(Androgen receptor) 0.829
NR-Aromatase 0.893
NR-ER(Estrogen receptor) 0.715
NR-ER-LBD(Estrogen receptor) 0.029

Allergy
Skin Sensitization Rule 1
Skin Sensitization 0.662

Acute Toxicity
Acute Toxicity Rule 4
Rat Oral Acute Toxicity 0.918

Organ Toxicity
hERG Blockers 0.017
H-HT(The human hepatotoxicity) 0.092
DILI(Drug-induced liver injury) 0.642

Primary Irritation
Eye Corrosion 0.046
Eye Irritation 0.063
Respiratory Toxicity 0.975

Mutagenic Effects
AMES Toxicity 0.671

Tumorigenic Effects
Carcinogencity 0.838
SR-ARE(Antioxidant Response Element) 0.041
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.444
SR-p53 0.957

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