99
5
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T21474 |
Navuridine
AZddU,CS 87,CS-87,AzUrd,3'-Azido-2',3'-dideoxyuridine,AZdU,3'-叠氮-2',3'-双脱氧尿苷 |
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
Navuridine (AZdU) 是一种口服活性的 HIV 逆转录酶抑制剂,半衰期相对较短。 | |||
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。 | |||
T33941 |
PF-03635659
PF03635659,PF 03635659 |
AChR | Neuroscience |
PF-03635659是一种强效且解离半衰期长的毒蕈碱M3拮抗剂(Ki:0.2 nM),显示出治疗慢性阻塞性肺病(COPD)的潜力。 | |||
T10392 |
Aspoxicillin
|
Anti-infection; Antibacterial | Microbiology/Virology |
Aspoxicillin 是一种广谱抗菌剂,对分离的胸膜肺炎放线杆菌 68 菌株抑制作用的MIC90值 ≤ 0.05 μg/ml。 | |||
T3967 |
Exendin-4
艾塞那肽,Exenatide,Exenatide Acetate |
Glucagon Receptor | GPCR/G Protein |
Exendin-4 (Exenatide) 是一种长效的 glucagon-likepeptide-1 受体激动剂(IC50: 3.22 nM),是一种由 39 个氨基酸组成的多肽。 | |||
T1223 |
Ceftriaxone sodium hydrate
Ceftriaxone Sodium Trihydrate,头孢曲松钠,Ceftriaxone disodium hemiheptahydrate,头孢曲松钠水合物,Ceftriaxone sodium |
Others; Antibacterial; Antibiotic | Microbiology/Virology; Others |
Ceftriaxone sodium hydrate 是一种头孢菌素类抗生素,对革兰氏阳性和革兰氏阴性菌均有活性。它具有抗炎和抗氧化作用。 | |||
T1410 |
Torsemide
AC-4464,JDL-464,托拉塞米,Torasemide |
Na-K-Cl cotransporter | Membrane transporter/Ion channel |
Torsemide (AC-4464) 是具有口服活性的亨氏环利尿剂,也具有抗醛固酮和血管舒张活性。它可用于研究心力衰竭、肾脏疾病、肝硬化。 | |||
T71708 |
Minamestane
|
Aromatase | Endocrinology/Hormones |
Minamestane 是一种新型不可逆芳香化酶抑制剂。Minamestane 引起人胎盘芳香化酶的时间依赖性抑制,半衰期为4分钟,K 为59nM。Minamestane 具有抗肿瘤活性。 | |||
T0195 |
Secnidazole
RP-14539,PM-185184,塞克硝唑 |
Antibiotic; Parasite | Microbiology/Virology |
Secnidazole (PM-185184) 是一种具有口服活性唑类抗生素,半衰期比甲硝唑更长。它有潜力研究细菌性阴道病。 | |||
T15300 |
Fluorofenidone
AKF-PD |
Others | Others |
Fluorofenidone (AKF-PD) 是 AMR69 的类似物,抗纤维化活性与 AMR69相同,但 Fluorofenidone 的毒性更低,半衰期长。它部分通过 PI3K/Akt 信号通路抑制 NADPH 氧化酶和细胞外基质 (ECM) 的沉积,能够减少肾间质纤维化的发生。 | |||
T60919 |
SARS-CoV-2-IN-13
|
SARS-CoV | Microbiology/Virology |
SARS-CoV-2-IN-13 (compound 6) 是氯硝柳胺的类似物。在人血浆和肝S9酶测定中,SARS-CoV-2-IN-13 比氯硝柳胺更稳定。SARS-CoV-2-IN-13 口服给药时可以提高生物利用度和半衰期。SARS-CoV-2-IN-13 是SARS-CoV-2的有效抑制剂,IC50值为 0.057 μM。 | |||
T15117 |
Didesmethyl cariprazine
|
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
Didesmethyl cariprazine 是 Cariprazine 的代谢物,是主要的循环活性部分。 Didesmethyl cariprazine 有较长的半衰期,为 1-3 周。Cariprazine 是一种有效的多巴胺D3偏好D3/D2受体部分激动剂,用于治疗精神分裂症、双相躁狂和抑郁症,对d3和d2受体具有高亲和力,对5-HT 1A 受体具有中等亲和力。 | |||
T60538 |
SARS-CoV-2-IN-14
3',5-Dichlorosalicylanilide |
SARS-CoV | Microbiology/Virology |
SARS-CoV-2-IN-14 是一种有效的、可口服的 SARS-CoV-2 抑制剂(IC50 :0.39 μM),是一种氯硝柳胺类似物。SARS-CoV-2-IN-14在人血浆和肝 S9 酶测定中比氯硝柳胺稳定性更强。SARS-CoV-2-IN-14以口服的方式给药可以提高其生物利用度和半衰期。 | |||
T3716 |
Rolapitant
罗拉吡坦,SCH619734,罗拉匹坦 |
Neurokinin receptor | GPCR/G Protein; Neuroscience |
Rolapitant (SCH619734) 是一种高效选择性具有口服活性的神经激肽 1 受体抑制剂,Ki 值为0.66 nM。 | |||
T2671 |
Regadenoson
CVT-3146,瑞加德松,Lexiscan |
Adenosine Receptor | GPCR/G Protein; Neuroscience |
Regadenoson (CVT-3146) 是一种腺苷衍生物和选择性 A2A 腺苷受体激动剂,具有冠状动脉舒张活性,对大鼠和猪腺苷 A2A 受体的Ki 分别为 290 和 1120 nM。它是血管扩张剂,可增加啮齿动物血脑屏障的通透性。 | |||
T8947 |
dasiglucagon acetate
dasiglucagon acetate(1544300-84-6 free base) |
Others | Others |
dasiglucagon acetate 是一种用于糖尿病低血糖治疗的新型胰高血糖素类似物。 它已证明在水性制剂中的溶解度和稳定性。药代动力学研究表明,与传统的重组胰高血糖素相比,它的胰高血糖素具有更高的吸收率和更长的血浆消除半衰期。 | |||
T35868 |
BCAT-IN-2
|
||
BCAT-IN-2 is a potent, selective and orally active inhibitor of mitochondrial branched-chain aminotransferase (BCATm), with a pIC50 of 7.3. BCAT-IN-2 shows selectivity for BCATm over BCATc (pIC50=6.6). BCAT-IN-2 can be used for the research of obesity and dislipidema[1]. BCAT-IN-2 (compound 61) inhibits BCATm in differentiated primary human adipocyte, with pIC50 of 6.5[1]. BCAT-IN-2 (compound 61) (10-100 mg/kg; p.o.) increases the level of leucine from 473 μM to 1.2 mM at the dose of 100 mg/kg i... | |||
TP1895L1 |
KYL acetate(676657-00-4 free base)
|
Ephrin Receptor | Tyrosine Kinase/Adaptors |
KYL acetate(676657-00-4 free base) 是EphA4受体酪氨酸激酶抑制剂(Kd = 0.8 μM);抑制 EphA4-EphrinA5 相互作用 (IC50 = 6.34 μM)。防止 AβO 诱导的突触损伤、树突棘丢失并防止海马 CA3-CA1 传输中 LTP 的阻断。在细胞培养基中表现出较长的半衰期(在 PC3 和 C2C12 培养基中分别为 8 和 12 小时)。它有神经保护作用。 | |||
T29075 |
UR-7247
UR7247 |
||
UR-7247 is an angiotensin type 1 receptor antagonist with a very long plasma elimination half-life. | |||
T24390 | LB-205 | ||
LB-205 is a Zn 2+ dependent pan-inhibitor of class I and class II HDACs. It also has a long half-life in vivo. | |||
T36510 |
V-PYRRO/NO
|
||
V-PYRRO/NO is a NO donor in vivo. Following hepatic metabolism, it spontaneously decomposes with a half-life of 3 seconds to liberate NO. | |||
T34590 |
SD-254
Venlafaxine deuterium-substituted,D9-venlafaxine |
||
SD-254 is a deuterium analog of Effexor, with fewer side effects and a longer half-life. | |||
T40239 |
Tenofovir-C3-O-C15-CF3 ammonium
Tenofovir-C3-O-C15-CF3 ammonium |
||
Tenofovir-C3-O-C15-CF3 (ammonium) demonstrates prolonged half-life values compared to tenofovir in human liver microsomes. It exhibits potent anti-HIV activity in vitro and enhances pharmacokinetic properties in vivo. | |||
T27374 |
FR-181877
FR181877,FR 181877 |
||
FR-181877, a nonprostanoid PGI2 agonist, inhibits ADP-induced aggregation of human platelets with an IC50 value of 0.081 microM and has high oral bioavailability (56%) with a long half-life (4.3 h) in rats. | |||
T40238 |
Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium
Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium |
||
Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) displays a prolonged half-life (t1/2) compared to tenofovir in human liver microsomes. Moreover, it demonstrates potent in vitro anti-HIV activity and improves in vivo pharmacokinetic properties. | |||
T36210 |
15-keto Treprostinil (sodium salt)
|
||
15-keto Treprostinil is an impurity found in treprostinil , which is a stable analog of prostaglandin I2 with a longer plasma half-life. Formulations containing treprostinil are used for the treatment of primary pulmonary hypertension. | |||
T34589 |
SD-1077
d3-L-DOPA,deuldopa,deuterated levodopa,SD1077 |
||
SD-1077, also known as d3-L-DOPA, is a deuterium containing levodopa. SD-1077 has been shown in preclinical models to improve the half-life of dopamine in the brain resulting in a prolonged treatment effect. | |||
T27141 |
Delimotecan
MEN4901,MEN 4901,T-0128,MEN-4901,T 0128 |
||
Delimotecan is a DNA topoisomerase I inhibitor. Delimotecan had a long terminal half-life of 109 h, and relatively high exposures to T-2513 and SN-38 were obtained. The percentage decrease in WBC and absolute neutrophil count significantly correlated with | |||
T35960 |
PROLI NONOate
|
||
PROLI NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 1.8 seconds at 37°C (pH 7.4) to liberate 2 moles of NO per mole of parent compound. | |||
T68563 |
Piroxicam olamine
|
||
Piroxicam olamine is a cyclooxygenase inhibiting, non-steroidal anti-inflammatory agent (NSAID) that is well established in treating rheumatoid arthritis and osteoarthritis and used for musculoskeletal disorders, dysmenorrhea, and postoperative pain. Its long half-life enables it to be administered once daily. | |||
T81826 | Meayamycin D | ||
Meayamycin D, 作为FR901464的类似物,能够诱导MCL-1的选择性剪接,并在小鼠血浆中展现出较长的半衰期。 | |||
T68345 |
GTS511
|
||
GTS511 is a EAAT2 Activator. Pharmacokinetic profiles (PK) of GTS511 show a >6 h half-life and higher bioavailability in plasma and the brain under all three routes of administration in rats. GTS511 can be further developed to treat neurological disorders caused by excitotoxicity | |||
T27799 |
LAS191859
LAS-191859,LAS 191859 |
||
LAS191859 is a CRTH2/DP2 antagonist with IC50 values of 7.6, 9.58, 14 and 15.5nM for recombinant guinea pig, human, rat and mouse CRTH2/DP2 receptors, respectively. LAS191859 has a residence time half-life of 21h at CRTh2 that translates into a long-lasti | |||
T62919 | CDK9-IN-13 | ||
CDK9-IN-13 是一种有效的、选择性的 CDK 抑制剂 (IC50<3 nM)。CDK9-IN-13 在啮齿动物中的半衰期很短。 | |||
T76930 | Bifarcept | ||
Bifarcept为一种针对干扰素受体I型(IFN-RI)的重组抗体,能与IFN-β结合,从而延长其在血清中的半衰期。 | |||
T74714 |
TP0597850
|
||
TP0597850为MMP2选择性抑制剂,展现出卓越的亲和力(IC50=0.22 nM)和较长的MMP2解离半衰期(t1/2=265 min)。 | |||
T36615 |
DPTA NONOate
Dipropylenetriamine NONOate |
||
DPTA NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of three hours and five hours at 37°C and 22-25°C, pH 7.4, respectively, to liberate 2 moles of NO per mole of parent compound. [1][2] | |||
T36546 |
Prostaglandin I3 (sodium salt)
Prostaglandin I3 (sodium salt) |
||
PGI3 is synthesized from EPA by COX and PGI synthase. PGI3 has a short in vivo half-life and is hydrolyzed to δ17-6-keto PGF1α. The platelet and vascular activity of PGI3 is equivalent to that of PGI2. | |||
T62855 |
OX2R-IN-1
|
||
OX2R-IN-1 是一种 OX2R 拮抗剂 (一种潜在的 OX2R 结合剂),表现出低细胞毒性 (IC50: 484 μM)。OX2R-IN-1 具有血脑屏障通透性,药物半衰期短。 | |||
T61639 |
S1P1 agonist 4
|
||
S1P1 agonist 4 在效价(EC50< 0.05 mg/kg)和预测人类半衰期方面都有更好的表现 (t1/2 ~ 5 天)。 | |||
T36177 |
Angeli’s Salt
Angeli’s Salt,Sodium α-oxyhyponitrite |
||
Angeli’s salt is regarded as a classical nitroxyl (NO-) donor, but under certain conditions evolution of NO is also observed.1 It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 2.3 minutes at 37°C (pH 7.4) to liberate 0.54 moles of NO per mole of parent compound.[1],[2] | |||
T68765 |
Spirorenone
|
||
Spirorenone is an androstadienone derivative as a highly effective aldosterone antagonist. Spirorenone is 8.6 times as potent as spironolactone, but showed a lower affinity for the mineralocorticoid receptors. In phase I clinical trials Spirorenone was absorbed with a half-life of 20-30 min, achieving maximum concentrations of about 100 ng/ml (10 mg) and 260 ng/ml (40 mg) after 1-2 h. Disposition of the parent drug was biphasic with half-lives of 50-60 min (distribution) and 5-6 h (elimination).... | |||
T78533 |
JG-23
|
||
JG-23是一种4-氯修饰类似物,能促进t-tau降解,并在小鼠肝微粒体检测中显示出良好的代谢稳定性,具备较长的半衰期(T1/2值为36分钟)。 | |||
T10589L |
BPN-15606
|
Others | Others |
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 has acceptable PK/PD properties, including bioavai | |||
T81525 |
Pegylated synthetic human c-peptide
|
||
Pegylated synthetic human c-peptide 保留与天然(即非聚乙二醇化)C 肽相当的生物活性,且延长了在血浆中的循环停留时间,适用于糖尿病性周围神经病变的研究。 | |||
T36239 |
6β-Prostaglandin I1
6β-Prostaglandin I1 |
||
6β-PGI1 is a stable PGI2 analog resistant to hydrolysis in aqueous solutions. 6β-PGI1 has a much longer half-life than PGI2, but a greatly reduced molar potency for receptor mediated function. 6β-PGI1 has a Kact for adenylate cyclase in NCB-20 cells of 4.2 μM compared with 18 nM for PGI2. The potency for vasodilation and inhibition of platelet aggregation is about 1% of PGI2. | |||
T69608 | TG11-77 HCl | ||
TG11-77 is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma half-life of 2.4 h in mice. TG11-77 are representative second generation EP2 antagonists with improved pharmacodynamic and pharmacokinetic properties. | |||
T35969 |
NOC-5
|
||
NOC-5 is a stable nitric oxide (NO)-amine complex that acts as a NO donor. It can release two equivalents of NO in solution under physiological conditions without a cofactor. [1] The half-life of NOC-5 in PBS (pH 7.4) is 93 minutes at 22°C, and it remains relatively stable in alkaline solution (pH >=10.0). [1] | |||
T69609 |
TG11-77 free base
|
||
TG11-77 is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma half-life of 2.4 h in mice. TG11-77 are representative second generation EP2 antagonists with improved pharmacodynamic and pharmacokinetic properties. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4814 |
(R)-5-Oxopyrrolidine-2-carboxylic acid
D-Pyroglutamic acid,(R)-(+)-2-Pyrrolidone-5-carboxylic acid,D-焦谷氨酸 |
Others; Endogenous Metabolite | Metabolism; Others |
(R)-5-Oxopyrrolidine-2-carboxylic acid (D-Pyroglutamic acid) 是内源性代谢产物的一种。 | |||
T4940 |
3-Methylhistamine dihydrochloride
|
Others; Endogenous Metabolite | Metabolism; Others |
3-Methylhistamine dihydrochloride 是一种组胺的降解产物,与免疫反应有关,并在接种过疫苗的小鼠中表现出上调作用。 | |||
T75661 | Thymopentin acetate | ||
Thymopentin acetate为胸腺皮质及髓质上皮细胞主要分泌的生物活性肽,是一有效免疫调节剂,具有极短的血浆半衰期(30秒),能促进自人类胚胎干细胞生成T细胞群。 | |||
TN2255 | Taccalonolide AJ | Others | Others |
Taccalonolide AJ is a microtubule stabilizer; it has excellent and highly persistent antitumor efficacy when administered directly to the tumor, suggesting that the lack of antitumor efficacy seen with systemic administration of AJ is likely due to its sh | |||
T37997 |
Murideoxycholic Acid
|
||
Murideoxycholic acid (MDCA) is a secondary bile acid produced from α-muricholic acid and β-muricholic acid.[1] It is also a metabolite of lithocholic acid in liver S9 fractions from humans and other species.[2] MDCA prevents gallstone formation in hamsters fed a lithogenic diet but does not resolve gallstones in prairie dogs fed a high cholesterol diet.[3],[4] Gallstones formed during MDCA administration after a high cholesterol diet are comprised of an insoluble calcium salt of murideoxycholyl ... |