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Cat. No. | Product Name | ||
---|---|---|---|
L1580 | GPCR库Plus | 338 compounds | |
338 种GPCR 靶向、结构新颖的化合物; | |||
L6810 | 中药单体化合物库 | 2755 compounds | |
2755 种中药来源的单体化合物,是药物开发、药理研究等领域的有力工具; | |||
L6800 | 中国药典收录天然产物库 | 2051 compounds | |
2051 种中国药典收录的天然产物,是药物开发、药理研究等领域的有力工具; | |||
L9900 | 药用辅料化合物库 | 182 compounds | |
182 种 FDA 批准药品中的非活性成分集合 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10480 | Bay 41-4109 (less active enantiomer) | HBV | Microbiology/Virology |
Bay 41-4109 less active enantiomer shows less activity than Bay 41-4109. BAY 41-4109 is a potent HBV inhibitor (IC50: 53 nM). | |||
T6352 |
(-)-Dizocilpine maleate
C13737,(-)-MK 801 (Maleate),(-)-MK 801马来酸,(-)-MK 801 Maleate |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) 是一种选择性且非竞争性的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂,Ki 为 211.7 nM。它是一种 Dizocilpine 的活性较低的 (-)-对映体,具有抗抑郁作用。 | |||
T12814 |
(S)-Tenofovir
(S)-替诺福韦,(S)-PMPA,(S)-GS 1278,(S)-TDF |
Others | Others |
(S)-Tenofovir ((S)-PMPA) 是Tenofovir 的活性较低的S-对映体,Tenofovir 是一种核苷酸逆转录酶抑制剂。 | |||
T12664 |
(Rac)-BRD0705
|
Others | Others |
(Rac)-BRD0705 是 BRD0705 的活性较低的外消旋体。 BRD0705 是一种有效的特异性 GSK3α 抑制剂。 | |||
T12831 |
SAR405 R enantiomer
|
Others | Others |
SAR405 R enantiomer 是一种 PIK3C3/Vps34 抑制剂,也是活性低于 SAR405 的对映体。 | |||
T10376 |
ARS-1630
|
Ras | GPCR/G Protein; MAPK |
ARS-1630 是一种突变型 K-ras G12C 抑制剂。 它是 ARS-1620 的活性较低的对映异构体。 | |||
T68051L |
RS 15385-198
|
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
RS 15385-198 是 Delequamine 的低活性异构体。Delequamine 是一种选择性 α2-肾上腺素受体拮抗剂。 | |||
T7080 |
CCT245737
SRA737 |
Chk | Cell Cycle/Checkpoint |
CCT245737 (SRA737) 是一种具有口服活性的选择性 Chk1 抑制剂,IC50值为 1.3 nM。 | |||
T9554 |
SN-008
|
STING | Immunology/Inflammation |
SN-008 是 SN-011 的低活性类似物,可作为阴性对照。 | |||
T11129L |
Duvelisib (R enantiomer) hydrochloride
IPI-145 R enantiomer HCl,Duvelisib (R enantiomer) hydrochloride(1261590-48-0 Free base),INK1197 R enantiomer HCl |
PI3K | PI3K/Akt/mTOR signaling |
Duvelisib (R enantiomer) hydrochloride (INK1197 R enantiomer HCl) 是 PI3K 抑制剂。Duvelisib (R enantiomer) hydrochloride 是 Duvelisib 的活性较低的对映体。 | |||
T22818 |
GSK9027
GR agonist 23a,GSK 9027,GSK-9027 |
Glucocorticoid Receptor | Endocrinology/Hormones |
GSK9027 (GR agonist 23a) 是一种非甾体糖皮质激素受体 (GR) 激动剂。GSK9027 (GR agonist 23a) 在2×GRE报告基因上对比地塞米松的活性属于部分激动剂,活性较地塞米松活性较弱。 | |||
T9042 |
Teriflunomide impurity 3
4-Amino-N-(4-trifluoromethylphenyl)benzamide |
COX | Immunology/Inflammation; Neuroscience |
Teriflunomide impurity 3 (4-Amino-N-(4-trifluoromethylphenyl)benzamide) 是一种选择性COX-1抑制剂,IC50为 30 µM。 | |||
T22450 |
Tyrphostin B44, (+) enantiomer
酪氨酸磷酸化抑制剂AG 835 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Tyrphostin B44, (+) enantiomer 是一种表皮生长因子受体 (EGFR) 激酶抑制剂,IC50 为 0.86 μM,活性低于 (-) 对映体。 | |||
T6205 |
AT7519
|
Apoptosis; GSK-3; CDK | Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
AT7519 是一种CDK 抑制剂,对 CDK1,CDK2,CDK4-CDK6 以及 CDK9 的IC50值分别为 210,47,100,13,170 和 <10 nM。 | |||
T67905 |
GS-829845
|
JAK; Drug Metabolite | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Metabolism; Stem Cells |
GS-829845 是一种 JAK1 抑制剂,是 Filgotinib 活性代谢物的主要成分,其效力比母体低约 10 倍且半衰期更长。 | |||
T16759 |
Ritanserin
利坦丝林,R 55667 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Ritanserin (R 55667) 是一种长效、高效、相对选择性、可口服的5-HT2受体拮抗剂,IC50值为 0.9 nM。 | |||
T12146 |
N-Desmethyl-Apalutamide
N-Desmethyl Apalutamide,N-去甲基阿帕鲁胺杂质 |
P450; Androgen Receptor | Endocrinology/Hormones; Metabolism |
N-Desmethyl-Apalutamide 是一种 Apalutamide 的活性代谢产物,主要由 CYP2C8 和 CYP3A4 介导形成。它是一种低活性的雄激素受体拮抗剂,其作用力是 Apalutamide 活性的三分之一。它是中等至强的CYP3A4和CYP2B6诱导剂,并具有优异的血浆蛋白结合浓度。 | |||
T6104 |
Cerdulatinib hydrochloride
Cerdulatinib,PRT2070,PRT062070 hydrochloride,PRT062070,PRT2070 hydrochloride |
MLK; c-Fms; Tyrosine Kinases; Hippo pathway; JAK; Syk | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Stem Cells; Tyrosine Kinase/Adaptors |
Cerdulatinib hydrochloride (PRT2070 hydrochloride) 是一种选择性可逆,具有口服活性、 ATP 竞争性的 SYK 和 JAK 的双重抑制剂,抑制 JAK1、2、3、SYK 和 Tyk2的 IC50值分别为12、6、8、32 和 0.5 nM。它可用于研究自身免疫性疾病和B 细胞恶性肿瘤。 | |||
T12695 |
RBN-2397
|
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
RBN-2397 是一种有效的、选择性的、具有口服活性的跨物种 NAD+ 竞争性 PARP7 抑制剂,IC50 小于 3 nM。它选择性结合 PARP7 ,Kd 为0.001 μM,可恢复干扰素 I 型信号转导,有用于晚期或转移性实体肿瘤的研究潜力。 | |||
T15545 |
ICA-27243
|
Potassium Channel | Membrane transporter/Ion channel |
ICA-27243 是选择性的,口服有效的 KCNQ2/Q3钾通道开放剂,EC50为 0.38 μM。对 KCNQ4 和 KCNQ3/Q5 的激活效果较差。它具有抗惊厥和抗癫痫作用。 | |||
T6458 |
CYC-116
噻氯匹定 |
VEGFR; FLT; CDK; S6 Kinase; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
CYC116是一种有效的极光激酶 A 和 B 的抑制剂,Ki 值分别为8和9 nM。 | |||
T21938 |
AS-041164
|
PI3K | PI3K/Akt/mTOR signaling |
AS-041164 是选择性的,具有口服活性的PI3Kγ亚型抑制剂,IC50=70 nM。它对 PI3Kα (IC50:240 μM),PI3Kβ (IC50:1.45 μM) 和 PI3Kδ (IC50:1.70 μM) 的活性较低。它具有抗炎活性。 | |||
T11991 |
Mefentrifluconazole
|
P450; Antifungal | Metabolism; Microbiology/Virology |
Mefentrifluconazole 是一种有效的、选择性的和具有口服活性的真菌 CYP51 (Kd= 0.5 nM) 抑制剂,但对人芳香酶的抑制活性较低,IC50值为0.92 μM。它是一种新型唑类衍生物,用作农用广谱抗真菌剂。 | |||
T13140 |
Umbralisib R-enantiomer
TGR-1202 R-enantiomer,RP5264 R-enantiomer |
PI3K | PI3K/Akt/mTOR signaling |
Umbralisib R-enantiomer (RP5264 R-enantiomer) 是 PI3K 的δ型抑制剂,是 TGR-1202 活性较低的对映体。Umbralisib R-enantiomer 对δ型 pi3激酶的 IC50,至少比抑制剂对其他 PI3K 亚型(A, β和γ)的 IC50低20倍。 | |||
T0932 |
Cefixime
FK-027,头孢克肟,Cefspan,Cefiximum,Cephoral,FR-17027,CL-284635 |
Antibacterial; Antibiotic | Microbiology/Virology |
Cefixime (FR-17027) 是一种头孢菌素类抗生素, 可研究一些细菌感染。 | |||
T20898 |
(R)-Propranolol hydrochloride
Dexpropranolol hydrochloride,(R)-(+)-Propranolol,盐酸普奈洛尔 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
(R)-Propranolol hydrochloride (Dexpropranolol hydrochloride) 是一种抗肾上腺素受体拮抗剂,是一种普萘洛尔的活性较低的对映体。Dexpropranolol 是一种非选择性的β-adrenergic receptor 拮抗剂,对 β1AR 和 β2AR 具有高亲和力。 | |||
T35528L |
TD52 dihydrochloride
TD52 dihydrochloride(1798328-24-1 Free base),TD52 2HCl |
Others | Others |
TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti... | |||
T15199 |
Edicotinib
JNJ-527,JNJ-40346527 |
c-Fms; FLT; CSF-1R; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Edicotinib (JNJ-527) 是能够透过血脑屏障的、口服具有活性的、选择性的CSF-1R 抑制剂 (IC50:3.2 nM)。它对 KIT (IC50:20 nM) 和 FLT3 (IC50:190 nM) 的抑制作用较小。它抑制小胶质细胞的扩张,减弱小胶质细胞的增殖和神经退行性变。它可用于研究阿尔茨海默病和类风湿性关节炎。 | |||
T4481 |
Tucidinostat
HBI-8000,Chidamide,西达本胺,CS 055 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Tucidinostat (Chidamide) 是一种 HDAC 抑制剂,对 HDAC1、HDAC2、HDAC3、HDAC10 有抑制活性 (IC50=95/160/67/78 nM)。Tucidinostat 具有抗肿瘤活性,可以用于治疗 T 细胞白血病-淋巴瘤。 | |||
T6446 |
Clevudine
L-FMAU,克拉夫定,Levovir |
HBV; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology |
Clevudine (Levovir) 是一种非自然 L-构型的核苷类似物,是一种与聚合酶结合的非竞争性抑制剂,具有较强的抗 HBV 活性,半衰期长,毒性低的特点。 | |||
T1995 |
Fedratinib
TG-101348,SAR 302503 |
Apoptosis; FLT; c-RET; JAK | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Fedratinib (TG-101348) 是一种 JAK2 抑制剂,具有选择性、ATP 竞争性和具有口服活性,抑制 JAK2 和 JAK2V617F 激酶 (IC50=3 nM)。Fedratinib 可诱导肿瘤细胞凋亡,并可用于骨髓增生性疾病的研究。 | |||
T60336 |
CCR4 antagonist 3-1
|
CCR | Immunology/Inflammation; Microbiology/Virology |
CCR4 antagonist 3-1 是一种具有较低活性的趋化因子受体 4 (CCR4) 拮抗剂,对 [125I]TARC (胸腺和活化调节趋化因子) 具有抑制作用,IC50 值为 1.7 μM。CCR4 antagonist 3-1 对放射标记的[125I]TARC和巨噬细胞来源的趋化因子(MDC) 与 CEM 细胞表面的CCR4 受体的结合有抑制作用, 并对 TARC 介导的 CEM 细胞的体外迁移有抑制作用,IC50 值为 6.4 μM。 | |||
T13438 |
(R,S)-Ivosidenib
(R,S)-AG-120 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
(R,S)-Ivosidenib is the less active enantiomer of Ivosidenib . | |||
T26371 |
(2S,3R)-LP99
|
Others | Others |
(2S,3R)-LP99 is a less active enantiomer of LP99. | |||
T13426L |
(3S,4S)-Tofacitinib
(3S,4S)-托法替尼 |
Others | Others |
(3S,4S)-Tofacitinib, a less active enantiomer of tofacitinib, is a Janus kinases inhibitor. | |||
T13450 |
(S)-GNE-140
|
Others | Others |
(S)-GNE-140 is the less active enantiomer of GNE-140. | |||
T13451 |
(S)-Mapracorat
(S)-ZK-245186,(S)-BOL-303242X |
Others | Others |
(S)-Mapracorat is a selective and less active agonist of glucocorticoid receptor. | |||
T11801 |
l-Atabrine dihydrochloride
|
Others | Others |
l-Atabrine dihydrochloride displays antiprion activity. l-Atabrine dihydrochloride is a less active enantiomer of quinacrine. | |||
T10564 |
(8R,9S)-Talazoparib
(8R,9S)-BMN-673,他拉唑帕利 (8R,9S) |
Others | Others |
(8R,9S)-Talazoparib is Talazoparib enantiomer , less active than Talazoparib on the inhibition of PARP1 (IC50: 144 nM). | |||
T26163 |
Rubradirin B
|
Others | Others |
Rubradirin B has an antibacterial activity similar to rubradirin, but the antibiotic is less active. | |||
T19549 | Ro18-5362 | Others | Others |
Ro18-5362 is the less active prodrug of Ro 18-5364. | |||
T12635 |
(R)-Plevitrexed
(R)-ZD 9331,(R)-BGC9331,(R)-普来曲塞 |
Others | Others |
(R)-Plevitrexed is a less active enantiomer of Plevitrexed. Plevitrexed is an orally active and potent inhibitor of thymidylate synthase (TS). | |||
T13427 |
(3S,4R)-Tofacitinib
|
Others | Others |
(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib is a JAK3 inhibitor(IC50 : 1 nM). | |||
T11156 |
Nazartinib S-enantiomer
EGF816 (S-enantiomer) |
Others | Others |
Nazartinib is an EGFR inhibitor. Nazartinib S-enantiomer is the less active S-enantiomer of Nazartinib. | |||
T6493L |
(R)-Citalopram oxalate
|
Others | Others |
(R)-Citalopram oxalate is a less active enantiomer of Escitalopram Oxalate. Escitalopram Oxalate is a potent and selective serotonin reuptake inhibitor. | |||
T12636 |
(R)-(+)-Anatabine
|
Others | Others |
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent agonist of α4β2 nAChR. | |||
T10856 |
Cobimetinib (R-enantiomer)
考比替尼 (R 型对映体),XL-518 R-enantiomer,Cobimetinib R-enantiomer,GDC-0973 R-enantiomer |
Others | Others |
Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib which is a selective MEK inhibitor. | |||
T12641 |
(R)-SCH 42495
|
Others | Others |
(R)-SCH 42495 is the less active enantiomer of SCH 42495. SCH 42495 is an orally active inhibitor of neutral metalloendopeptidase (NEP), with antihypertensive effect. | |||
T15186 |
(E)-4-Hydroxytamoxifen
|
Others | Others |
(E)-4-Hydroxytamoxifen is a less active isomer of (Z)-4-hydroxytamoxifen and also is an estrogen receptor modulator. | |||
T11335 |
Fulvestrant (S enantiomer)
ZM 182780 S enantiomer,ICI 182780 S enantiomer,Fulvestrant S enantiomer,ZD 9238 S enantiomer |
Others | Others |
Fulvestrant S enantiomer is the less active S enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T20191 |
(-)-Camphoric acid
(-)-樟脑酸,L-Camphoric acid,Camphoric acid, (-)- |
GluR | Neuroscience |
(-)-Camphoric acid (L-Camphoric acid) 是一种活性较低的樟脑酸对映异构体,樟脑酸可诱导 GluR 表达。 | |||
T13669 |
(E)-Cinnamamide
trans-Cinnamamide,肉桂酰胺 |
Others | Others |
(E)-Cinnamamide (trans-Cinnamamide) 是 Cinnamamide 的活性较低的异构体,Cinnamamide 是一种有效的非致命化学驱虫剂,适用于减少鸟类害虫的损害。 | |||
TN1448 |
(-)-Bornyl acetate
L-(-)-Bornyl acetate,左旋乙酸冰片酯,Bornyl acetate,(-)-乙酸龙脑酯 |
p38 MAPK; NF-κB; JNK; Antifungal | MAPK; Microbiology/Virology; NF-κB |
(-)-Bornyl acetate (L-(-)-Bornyl acetate) 是存在于牛膝草油中的一种具有抗真菌活性的 (+)-Bornyl acetate 低活性异构体。 | |||
T36585 |
Isodeoxycholic Acid
isoDCA |
Chloride channel; Antibacterial | Membrane transporter/Ion channel; Microbiology/Virology |
Isodeoxycholic Acid 是一种胆汁酸,由肠道细菌通过脱氧胆酸的表聚作用形成。Isodeoxycholic acid 的临界胶束浓度高于二氯苯甲醚,这表明它的去污活性降低了,而且在抑制七种肠道共生细菌生长方面的活性低于二氯苯甲醚。Isodeoxycholic Acid(0.1%)能抑制几种艰难梭菌菌株在牛磺胆酸诱导下的孢子萌发,并能降低艰难梭菌培养上清对 Vero 细胞的细胞毒性。在高脂饮食诱发肥胖的大鼠模型中,血浆中的Isodeoxycholic acid 水平比正常饮食的大鼠低。 | |||
TN2931 |
3-Epikatonic acid
|
Antifection | Microbiology/Virology |
Epikatonic acid shows less active against T. (S.) cruzi trypanosome. | |||
T38497 |
(-)-Taxifolin
(-)-二氢槲皮素,(-)-Dihydroquercetin |
Others | Others |
(-)-Taxifolin is the less active enantiomer of Taxifolin, demonstrating vital anti-tyrosinase activity and notable inhibition against collagenase (IC50 = 193.3 μM). It is valued as an essential natural compound showing antifibrotic potential, while also acting as a capable free radical scavenger and possessing antioxidant capacity. | |||
TN4471 |
Lysicamine
|
IL Receptor; Antifection | Immunology/Inflammation; Microbiology/Virology |
Lysicamine shows significant antioxidant capacity in the ORAC(FL) assay and it is active against S. epidermidis and C. dubliniensis, with MIC values in the range 12.5-100 microg mL(-1). Lysicamine has antimicrobial and anti-inflammation activity, the mini |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-02778 |
Mcpt4 Protein, Mouse, Recombinant (E. coli, His)
MSMCP,Mast cell protease 4,Myonase,Serosal mast cell proteas... |
Mouse | E. coli |
Has chymotrypsin-like activity. Hydrolyzes the amide bonds of synthetic substrates having Tyr and Phe residues at the P1 position. Preferentially hydrolyzes the 'Tyr-4-|-Ile-5' bond of angiotensin I and the 'Phe-20-|-Ala-21' bond of amyloid beta-protein, and is less active towards the 'Phe-8-|-His-9' bond of angiotensin I and the 'Phe-4-|-Ala-5' and 'Tyr-10-|-Glu-11' bonds of amyloid beta-protein. Involved in thrombin regulation and fibronectin processing. Mcpt4 Protein, Mouse, Recombinant (E. c... | |||
TMPJ-01320 |
BSSP-4 Protein, Human, Recombinant (His)
BSSP4,Tryptase ε,Serine Protease 26,BSSP-4,Serine Protease 2... |
Human | HEK293 Cells |
Brain-Specific Serine Protease 4 (BSSP-4) is a serine protease that preferentially cleaves the synthetic substrate H-D-Leu-Thr-Arg-pNA compared to tosyl-Gly-Pro-Arg-pNA. BSSP-4 is expressed abundantly in the epithelial cells of the airways, including trachea, esophagus and fetal lung, but scarce in adult lung and expressed at low levels in placenta, pancreas, prostate and thyroid gland. BSSP-4 belongs to the peptidase S1 family and related to trypsin, referentially hydrolyzing substrates after a... | |||
TMPJ-00052 |
Leptin Protein, Mouse, Recombinant
OB,Obesity Factor,OBS,LEP,Obese Protein,Leptin |
Mouse | E. coli |
Leptin is a hormone secreted from white adipocytes and plays important role in the regulation of food intake and energy balance. Leptin functions via signaling pathways involving OB-R in hypothalamus. Animal models have revealed the influence of Leptin in reducing body weight and regulating blood glucose level. When mutations are introduced in obese gene, mice with impaired function of leptin are massively obese and in high risk of diabetes. Leptin deficiency reduces metablic rate. Leptin defici... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMIH-0372 |
N-desmethyl Apalutamide-d4
|
||
N-desmethyl Apalutamide-d4 是 N-desmethyl Apalutamide 的氘代化合物。N-desmethyl Apalutamide 的 CAS 号为 1332391-11-3。N-Desmethyl Apalutamide 是一种 Apalutamide 的活性代谢产物,主要由 CYP2C8 和 CYP3A4 介导形成。它是一种低活性的雄激素受体拮抗剂,其作用力是 Apalutamide 活性的三分之一。它是中等至强的CYP3A4和CYP2B6诱导剂,并具有优异的血浆蛋白结合浓度。 |