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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1973 |
PFI-4
PFI4 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
PFI-4是一种可渗透细胞的选择性BRPF1溴结构域抑制剂,IC50为 80 nM,作用于BRPF1比作用于其他溴结构域选择性强 100 多倍。 | |||
T21616 |
L-006235
L 006235 |
Cysteine Protease | Proteases/Proteasome |
L-006235 是一种口服有活性的、可逆的cathepsin K 选择性抑制剂,在骨吸收试验中的IC50值为 5 nM。它能够抑制胶原蛋白降解,并较少骨质流失。 | |||
T1867 |
Otenaproxesul
ATB 346 |
Apoptosis; COX | Apoptosis; Immunology/Inflammation; Neuroscience |
Otenaproxesul (ATB 346) 是一种具有口服活性的非甾体抗炎药,可抑制环氧合酶-1 和 2,具有抗炎生物活性,可用于缓解疼痛的研究。 | |||
T2188 |
Thonzonium Bromide
嘧苯十六铵,通佐溴胺 |
Proton pump; Antibacterial; Autophagy | Autophagy; Membrane transporter/Ion channel; Microbiology/Virology |
Thonzonium bromide 是一种单阳离子表面活性剂,在结构上与 Farnesol 相似的抗菌剂。它以剂量依赖的方式抑制质子转运 (EC50=69 μM)。在体外可抑制 RANKL 诱导的破骨细胞形成和骨吸收,并在体内阻止 LPS 诱导的骨丢失。 | |||
T11098 |
Droloxifene
3-Hydroxytamoxifen |
Estrogen Receptor/ERR | Endocrinology/Hormones |
Droloxifene (3-Hydroxytamoxifen),Tamoxifen 衍生物,是一种具有口服活性和选择性的雌激素受体 (estrogen receptor) 调节剂。Droloxifene 具有抗雌激素和抗植入作用。Droloxifene 诱导 MCF-7 细胞 p53 表达及凋亡。Droloxifene 预防去卵巢大鼠骨丢失。 | |||
T61317 | Anabolic agent-1 | ||
Anabolic agent-1 is a novel bone morphogenetic protein-2 up regulator, with the capability of rectifying bone loss in patients and exhibiting versatile clinical applicability. | |||
T26512 | ABD-295 | ||
ABD-295 is an antiresorptive agent, osteoclast inhibitor, and biphenylsulfide derivative. ABD-295 has potent inhibitory effects on osteoclastic bone resorption in vitro. ABD-295 prevents ovariectomy-induced bone loss in vivo. | |||
T69793 | VEL-0230 | ||
VEL-0230, also known as NC-2300, is a potent cathespin K inhibitor. VEL-0230 has dual-acting properties that both stimulates bone formation and inhibits loss. VEL-0230 is being studied preclinically for the treatment of diseases involving bone mineral disorders such as bone loss related to multiple myeloma, osteoporosis, bone metastases, and rheumatoid arthritis. Velcura Therapeutics is currently being developed by Velcura Therapeutics. Given VEL- 0230's promotion of bone formation, inhibition o... | |||
T69656 | E197 | ||
E197 is a DOCK5 inhibitor. E197 can inhibit both mouse and human osteoclast activity. In particular, E197 prevented pathological bone loss in mice. Most interestingly, treatment with E197 did not affect osteoclast and osteoblast numbers and hence did not impair bone formation. E197 could represent a lead molecule to develop new antiosteoporotic drugs targeting the mechanism of osteoclast adhesion onto the bone. | |||
T40245 |
Miroestrol
|
||
Miroestrol is a potent phytoestrogen compound with multifaceted biological effects. It induces a mammogenic effect and demonstrates neuroprotective properties, along with the ability to prevent bone loss in ovariectomized mice. Additionally, Miroestrol has been shown to reduce the risk of cancer [4]. | |||
T73770 | Galactosylhydroxylysine hydrochloride | ||
Galactosylhydroxylysine hydrochloride, 一种羟基赖氨酸经糖基化转换后生成的骨胶原蛋白成分,该化合物在骨吸收过程中释放,其浓度在代谢性骨丢失疾病中会上升。 | |||
T27968 |
M-5011
T-3788,S-MTPPA,M 5011,M-5011C |
||
M-5011 is a non-steroidal anti-inflammatory drug and immunomodulator potentially for the treatment of inflammation and pain. M-5011 had an effective antinociceptive activity (ED50 value) of 0.63 mg/kg. M-5011 partially inhibits the generalized bone loss a | |||
T10187 |
6-Raloxifene-β-D-glucopyranoside
|
Others | Others |
6-Raloxifene-β-D-glucopyranoside is a benzothiophene glucuronidated at the 6' position. It is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss, resorption, and lowering lipid | |||
T36080 |
Rivenprost
ONO-4819 |
||
Prostaglandin E2 activates four distinct G protein-coupled receptors, EP1-4. Rivenprost is a potent and selective agonist for the EP4 receptor (Ki = 0.7, 56, 620, and >10,000 nM for EP4, EP3, EP2, and EP1, respectively). It has been used to promote EP4-mediated bone formation, prevent bone loss related to osteoporosis, drive osteoblast differentiation, and stabilize bone implants.[1][2][3][4][5] Rivenprost has also been used to support wound healing.[6] | |||
T36127 |
TNF-α Antagonist
|
||
TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with the receptor. By blocking the TNF receptor ligand contact site, this peptide interferes with both activating receptor activator of NF-κB (RANK) and TNF-α's recruitment and activation of osteoclasts. TNF-α antagonist has been used to block bone resorption in the study of systemic bone loss in rheumatoid arthritis and inflammatory bone destr... | |||
T83848 |
VnP-16 TFA
|
||
VnP-16是一种合成肽段,对应vitronectin的氨基酸270-281,vitronectin是一种具有细胞附着、迁移和扩散等多功能作用的糖蛋白。该肽段在9.1 µg/cm2浓度下应用于细胞板时,能促进人类成骨细胞的附着和扩散,此效应可通过β1整合素的siRNA敲除被逆转。VnP-16诱导人类皮肤来源的间充质前体细胞和MC3T3-E1小鼠颅骨成骨前体细胞的成骨作用。在体内,VnP-16减少IL-1α诱导的骨质流失并减少小鼠颅骨中破骨细胞的数量。它还在卵巢切除引起的骨质疏失小鼠模型中增加骨矿物质密度并减少松质骨流失。 | |||
T30855L | CGP77675 hydrate | ||
CGP77675 hydrate 是一种口服有效的Src 家族激酶抑制剂。CGP77675 hydrate 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC50分别为 5-20 和 40 nM),并且还抑制 Src,EGFR,KDR,v-Abl 和 Lck,IC50分别为 0.02、0.15、1.0、0.31 和 0.29 μM。CGP77675 hydrate 可用于治疗与骨质流失相关的疾病,并具有抗肿瘤活性。 | |||
T40274 |
XVA143
XVA143 |
||
XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo. XVA143 is an antagonist of both mouse and human CR3, inhibits the ability of P. gingivalis to persist in the mouse host and cause periodontal bone loss. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5S2129 |
Sciadopitysin
|
TNF; NF-κB | Apoptosis; NF-κB |
Sciadopitysin 是一种双黄酮类化合物,来自银杏叶片中。它通过抑制NF-κB 活化并降低c-Fos 和NFATc1的表达来抑制 RANKL 诱导的破骨细胞生成和骨丢失。 | |||
T5575 |
Cycloastragenol
环黄芪醇,Cyclogalegenol,Astramembrangenin |
Epigenetic Reader Domain; Telomerase | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Cycloastragenol (Astramembrangenin) 是一种三萜皂苷类化合物,是黄芪主要活性成分的水解产物,具有抗氧化、抗炎、抗衰老、抗凋亡和心血管保护作用。它是端粒酶激活剂,可以延长端粒,还能缓解与年龄相关的骨丢失,改善骨微结构和生物力学特性。 | |||
TN1494 |
Cimicifugoside H-1
黑升麻苷H-1 |
Others | Others |
Cimicifugoside H1 是C. foetidaL.C 提取物的主要成分,是一种环甾烷醇木糖苷。它对骨吸收及卵巢切除术引起的骨质流失具有抑制作用。 | |||
TJS0856 |
Dalbergin
黄檀素,6-Hydroxy-7-Methoxy-4-Phenylcoumarin |
Others | Others |
Dalbergin (6-Hydroxy-7-Methoxy-4-Phenylcoumarin) 是一种 Dalbergia Sissoo Linn. knot wood 提取物的成分。它具有强大的抗氧化活性。 | |||
T6S0139 |
Neobavaisoflavone
|
Apoptosis; DNA/RNA Synthesis | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
Neobavaisoflavone 是一种从Psoralea corylifolia 的种子中分离出来的类黄酮。它具有抗炎,抗癌和抗氧化的作用。它在中至高浓度下可抑制 DNA 聚合酶,也可抑制血小板聚集。 | |||
T6S1966 |
Curculigoside
Curculigoside A,仙茅苷 |
Antioxidant; NF-κB; JAK; STAT | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; NF-κB; oxidation-reduction; Stem Cells |
Curculigoside (Curculigoside A) 是仙茅中的主要皂苷,具有显著的抗氧化、抗骨质疏松、抗抑郁和神经保护作用。它通过调节JAK/STAT/NF-κB 信号传导途径,具有抗关节炎作用。 | |||
T3849 |
Kinsenoside
金线莲苷,(+)-Kinsenoside |
Apoptosis; Nrf2 | Apoptosis; Immunology/Inflammation |
Kinsenoside ((+)-Kinsenoside) 是从金盏花属植物中分离得到的主要活性成分,以 Nrf2 依赖的方式保护髓核细胞在氧化应激下的生存能力,防止细胞凋亡、衰老和线粒体功能障碍。它显示出显着的抗肝毒性和抗炎活性。 | |||
T4S0969 |
Obtusifolin
决明蒽醌,决明蒽醌;美决明子素 |
Antioxidant; NF-κB | NF-κB; oxidation-reduction |
Obtusifolin 是分离自决明子的种子中,能够抑制NF-kB 通路,调节气道上皮细胞中 MUC5AC 粘蛋白的基因表达和产生。它通过靶向甲状旁腺激素相关蛋白来抑制邻苯二甲酸酯诱导的乳腺癌骨转移。 | |||
T3673 |
Mollugin
大叶茜草素,Rubimaillin |
HER; JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Mollugin (Rubimaillin) 是Rubia cordifolia L.中主要的生物活性成分。它能通过 p38-Smad 信号通路增强 BMP-2 的成骨作用。它通过抑制 TNF-α 诱导的 NF-κB 激活起抗癌疗效。 | |||
TN1778 |
Isoformononetin
异刺芒柄花素,黄豆苷元杂质 |
IL Receptor; Antifection | Immunology/Inflammation; Microbiology/Virology |
Isoformononetin shows fungitoxic activity against Cladosporium sphaerospermum; it also has immunomodulatory activity, it inhibits the differentiation of Th17 cells and B-cell lymphopoesis to promote osteogenesis in estrogen-deficient bone loss conditions. | |||
TN3754 |
Dalbergiphenol
檀木 |
Others | Others |
Dalbergiphenol shows antiosteoporotic activity, dalbergiphenol treatment can effectively prevent OVX-induced increase in bone loss and decrease in bone strength possibly by increasing osteoblastic activities and by decreasing osteoclastic activities. | |||
TN3802 |
Dehydrodiconiferyl alcohol
|
Estrogen/progestogen Receptor | Endocrinology/Hormones |
Dehydrodiconiferyl alcohol (DHCA) 是一种从葫芦中分离出来的木脂素,通过作为雌激素受体激动剂抑制破骨细胞分化和卵巢切除术诱导的骨质流失。 |