Ingredient Details :6-hydroxy-7-methylidene-1-[(2S,3R,4R,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4a,5,6,7a-tetrahydro-1H-cyclopenta[c]pyran-4-carboxylic acid


TCMI-ID: TCMI17262


Physicochemical Property
Ingredient Name 6-hydroxy-7-methylidene-1-[(2S,3R,4R,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4a,5,6,7a-tetrahydro-1H-cyclopenta[c]pyran-4-carboxylic acid
Pubchem CID 22524229
Iupac name 6-hydroxy-7-methylidene-1-[(2S,3R,4R,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4a,5,6,7a-tetrahydro-1H-cyclopenta[c]pyran-4-carboxylic acid
Molecular Formula C16H22O10
Molecular Weight 374.34
Isomeric smiles C=C1C(CC2C1C(OC=C2C(=O)O)O[C@H]3[C@@H]([C@@H]([C@H]([C@H](O3)CO)O)O)O)O
InChI InChI=1S/C16H22O10/c1-5-8(18)2-6-7(14(22)23)4-24-15(10(5)6)26-16-13(21)12(20)11(19)9(3-17)25-16/h4,6,8-13,15-21H,1-3H2,(H,22,23)/t6?,8?,9-,10?,11+,12-,13-,15?,16+/m1/s1
InChIKey JSKCJJNYSGWZDU-BXSUZMQKSA-N
External Database Links
Structural Information
nHA(Number of hydrogen bond acceptors) 10
nHD(Number of hydrogen bond donors) 6
nRot(Number of rotatable bonds) 4
nRing(Number of rings) 3
MaxRing(Number of atoms in the biggest ring) 9
nHet(Number of heteroatoms) 10

Stability
nRig(Number of rigid bonds) 18
Flexibility 0.222
Stereo Centers(Number of stereocenters) 9

Solubility
TPSA(Topological polar surface area) 166.14
logS(The logarithm of aqueous solubility value) -0.29
logP(The logarithm of the n-octanol/water distribution coefficient) -1.39
logD7.4(The logarithm of the n-octanol/water distribution coefficients at pH=7.4) -1.145

Pharmacokinetic Property
Quantitative Estimate of Drug-likeness 0.294
Synthetic accessibility score 4.827
Natural Product-likeness score 3.006
Lipinski Rule Accepted
GSK Rule Accepted
Golden Triangle Accepted

Absorption
Caco-2 Permeability -6.461
MDCK Permeability 0.000144919
Pgp-substrate 0.788
HIA(human intestinal absorption) 0.912
F20%(20% Oral Bioavailability) 0.345
F30%(30% Oral Bioavailability) 0.998

Distribution
PPB(Plasma protein binding) 35.83%
VD(Volume Distribution) 0.299
BBB Penetration(Blood brain barrier penetration) 0.229
B3 Penetration(Blood brain barrier penetration) Non-Permeable
Fu(The fraction unbound in plasms) 62.46%

Metabolism
CYP1A2 inhibitor 0.012
CYP1A2 substrate 0.016
CYP2C19 inhibitor 0.021
CYP2C19 substrate 0.055
CYP2C9 inhibitor 0.006
CYP2C9 substrate 0.067
CYP2D6 inhibitor 0.014
CYP2D6 substrate 0.098
CYP3A4 inhibitor 0.008
CYP3A4 substrate 0.029

Excretion
CL(The clearance of a drug) 1.565
T1/2 0.684

Toxicology
NonBiodegradable Rule 1
Pfizer Rule Accepted
SR-MMP 0.139

Toxic Dose
FDAMDD(FDA Maximum (Recommended) Daily Dose) 0.287
IGC50 1.797
LC50FM 2.573
LC50DM 3.644

Reproductive Effects
NR-AR(Androgen receptor) 0.021
NR-AR-LBD(Androgen receptor) 0.165
NR-Aromatase 0.002
NR-ER(Estrogen receptor) 0.088
NR-ER-LBD(Estrogen receptor) 0.02

Allergy
Skin Sensitization Rule 1
Skin Sensitization 0.048

Acute Toxicity
Acute Toxicity Rule 4
Rat Oral Acute Toxicity 0.346

Organ Toxicity
hERG Blockers 0.025
H-HT(The human hepatotoxicity) 0.364
DILI(Drug-induced liver injury) 0.922

Primary Irritation
Eye Corrosion 0.003
Eye Irritation 0.025
Respiratory Toxicity 0.633

Mutagenic Effects
AMES Toxicity 0.063

Tumorigenic Effects
Carcinogencity 0.923
SR-ARE(Antioxidant Response Element) 0.022
SR-ATAD5(ATPase family AAA domain-containing protein 5) 0.04
SR-p53 0.01

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