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Search Results for " osteoclasts "

19

抑制剂 & 化合物

7

天然产物

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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。
T9824	WAY-325371	Others	Others
	WAY-325371可抑制破骨细胞的形成。
T21460	Teriparatide acetate hPTH 1-34 (acetate salt),Parathar acetate,Forteo,醋酸立特帕肽	Others	Others
	Teriparatide acetate (Forteo) 是一种 PHT 激动剂，在 HEK293 细胞中的 IC50 为 2 nM。Teriparatide acetate 是一种重组形式的甲状旁腺激素。它是一种有效的合成代谢（即骨骼生长）剂，用于治疗某些形式的骨质疏松症。间歇使用特立帕肽比破骨细胞更能激活成骨细胞，从而导致骨骼整体增加。
T1210	Sodium etidronate 依替膦酸钠,Didronel	Phosphatase	Metabolism
	Sodium etidronate (Didronel) 是一种内源性 pyrophosphate 的合成治疗性 diphosphonate 类似物。作为称为 bisphosphonates 盐类药物家族的一员，etidronate disodium 与内源性 pyrophosphate 的不同之处在于其对酶水解的耐受性。该药剂吸附 hydroxyapatite 细胞并减少破骨细胞的数量，从而抑制异常骨吸收。 Etidronate 还可以直接刺激成骨细胞的骨形成。
T1641	Strontium ranelate Distrontium renelate,S12911,雷尼酸锶	Calcium Channel; CaSR	GPCR/G Protein; Membrane transporter/Ion channel; Metabolism
	Strontium ranelate (S12911) 是抗骨质疏松的药物，能够抑制骨吸收，促进骨形成，进而促使正骨平衡。它还能够激活非骨骼细胞中的钙敏感受体 (CaSR)，进而促进肌醇 1，4，5-三磷酸的生成及丝裂原活化的蛋白激酶信号转导。
T20338	Methopterin NSC 107144,alpha-Methopterin,NSC-107144,10-Methylfolic acid,NSC107144
	Methopterin shows the activation and bone resorption function of murine osteoclasts.
T22559	Alendronate sodium	Others	Others
	The compound binds and blocks farnesyl diphosphate synthase in the HMG-CoA pathway (IC50 = 460 nM for recombinant human FPPS). It causes macrophage apoptosis and inhibits prenylation and sterol biosynthesis in purified osteoclasts.
T21330	JNJ-28312141 JNJ 28312141,JNJ28312141
	JNJ-28312141 is an orally active CSF1R inhibitor and a FLT3 inhibitor. JNJ-28312141 is a new agent with potential therapeutic activity in acute myeloid leukemia and in settings where CSF-1-dependent macrophages and osteoclasts contribute to tumor growth a
TP2098	Echistatin Echistatin, α1 isoform
	Potent irreversible αVβ3 integrin antagonist (Ki = 0.27 nM). Disrupts attachment of osteoclasts to bone and inhibits bone reabsorption (IC50 = 0.1 nM). Prevents ADP-induced platelet aggregation via inhibition of glycoprotein IIb/IIIa (GpIIb/IIIa, αIIbβ3)
T68721	Cantharidin imide
	Cantharidin imide is a PP1/2A inhibitor found in Canarthis vesicatoria. It inhibits proliferation of colorectal cancer cells, increases MCP-1, IL-6, and IL-β levels, and inhibits differentiation and resorptive activity of osteoclasts. This compound can produce severe skin inflammation, and is extremely toxic if ingested orally.
T62189	sRANKL-IN-1
	sRANKL-IN-1 (compound S3) 是一种 sRANKL (soluble RANKL) 的抑制剂。sRANKL-IN-1 能够较强的抑制破骨细胞 (IC50: 0.096 μM，Kd: 34.80 μM)。sRANKL-IN-1 能够用于研究骨质疏松症。
T36065	N-Oleoyl-L-Serine
	Bone mass and shape is continuously remodeled by the concerted and balanced action of osteoblasts (bone forming cells) and osteoclasts (bone-resorbing cells). The endocannabinoid system plays an essential role in the maintenance of normal bone mass via signaling through the CB2 receptor. N-Oleoyl-L-serine is an endogenous lipid that has been reported to stimulate bone formation and to inhibit bone resorption.
T19848	Cyclosporin B 7-L-Alanine-cyclosporin A,Antibiotic S 7481F2
	Cyclosporin B is an immunosuppressant that has revolutionized organ transplantation through its use in the prevention of graft rejection. Cyclosporin B displays antiviral properties, inhibiting the entry of hepatitis B into hepatocytes. Cyclosporin B also
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...
T78816	Anti-osteoporosis agent-4	NF-κB	NF-κB
	Anti-osteoporosis agent-4 (Compound 11h) 在生物医学领域中表现为有效抑制原代破骨细胞的分化，减弱RANKL诱导的破骨细胞生成，并展示出强抑制作用，具有 IC50 值为358.29 nM。此外，该化合物还能抑制关键的 PI3K/AKT 和 IκBα/NF-κB 信号通路激活，表明其在防治骨质疏松症中的潜在应用价值。
T40463	Relacatib SB-462795
	Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V. It exhibits high affinity for these enzymes, with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Moreover, Relacatib effectively inhibits endogenous cathepsin K in situ in human osteoclasts, as well as human osteoclast-mediated bone resorption, with IC 50 values of 45 nM and 70 nM, respectively. Additionally, in vitro studies demonstrate Relacatib's inhibitory effect on bone resorption in ...
TP2049	CRSP-1
	Endogenous central calcitonin (CT) receptor agonist that stimulates cAMP formation at a potency 350-fold greater than CT (ED50 values are 0.2 and 71 nM respectively). Displays no activity at calcitonin-gene related peptide (CGRP) and adrenomedullin recept
T29542	AC708 AC 708,AC-708
	AC708 is a small molecule CSF1R inhibitor that effectively inhibits CSF1R phosphorylation mediated by CSF-1 (IC50 = 26 nM) and IL-34 (IC50 = 33 nM). It also inhibited the activity of growth factor-dependent cells cultured in CSF-1 (IC50 = 38 nM) or IL-34
T37413	Calcitonin (salmon) (trifluoroacetate salt)
	Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin. The binding of salmon calcitonin to the human calcitonin receptor (CTR) is not modulated by receptor activity-modifying proteins (RAMPs), which influence affinity of human calcitonin to CTR. Salmon calcitonin binds to human CTR2 with IC50 values of 0.933, 0.224, 0.134, and ...

化合物

Cat.No: T1973

Synonym: PFI4

Target: Epigenetic Reader Domain

Cat.No: T9824

Target: Others

Teriparatide acetate

Cat.No: T21460

Synonym: hPTH 1-34 (acetate salt),Parathar acetate,Forteo,醋酸立特帕肽

Target: Others

Sodium etidronate

Cat.No: T1210

Synonym: 依替膦酸钠,Didronel

Target: Phosphatase

Strontium ranelate

Cat.No: T1641

Synonym: Distrontium renelate,S12911,雷尼酸锶

Target: Calcium Channel, CaSR

Cat.No: T20338

Synonym: NSC 107144,alpha-Methopterin,NSC-107144,10-Methylfolic acid,NSC107144

Alendronate sodium

Cat.No: T22559

Target: Others

Cat.No: T21330

Synonym: JNJ 28312141,JNJ28312141

Cat.No: TP2098

Synonym: Echistatin, α1 isoform

Cantharidin imide

Cat.No: T68721

Cat.No: T62189

N-Oleoyl-L-Serine

Cat.No: T36065

Cat.No: T19848

Synonym: 7-L-Alanine-cyclosporin A,Antibiotic S 7481F2

TNF-α Antagonist

Cat.No: T36127

Anti-osteoporosis agent-4

Cat.No: T78816

Target: NF-κB

Cat.No: T40463

Synonym: SB-462795

Cat.No: TP2049

Cat.No: T29542

Synonym: AC 708,AC-708

Calcitonin (salmon) (trifluoroacetate salt)

Cat.No: T37413

Cat. No.	Product Name	Target	Signaling Pathways
T3808	Icariside I 淫羊藿次苷I,Lcariside I,Icariin I,Icarisid I	Others	Others
	Icariside I (Lcariside I) 是一种 Icarlin 的代谢产物，具有调节骨重塑的作用，可用于研究骨质疏松。
T5770	Alisol B	RANKL/RANK	NF-κB
	Alisol B 是一种具有用于骨科疾病研究潜力的化合物，通过分化破骨细胞发挥其功能。
T2789	Scutellarin 黄岑素,野黄芩苷,Breviscapin,Breviscapinun,Breviscapine,Scutellarein-7-glucuronide	Akt; HIV Protease; STAT	Cytoskeletal Signaling; JAK/STAT signaling; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
	Scutellarin (Scutellarein-7-glucuronide) 是从黄芩中分离的黄酮，可抑制破骨细胞中 RANKL 介导的 MAPK 和 NF-κB 信号通路，并下调 HCC 细胞中的 STAT3/Girdin/Akt 信号通路。
TN5888	Toddaculin	Others	Others
	Toddaculin 是一种天然香豆素，抑制过度的破骨细胞活性并增强成骨细胞分化和矿化。它可诱导白血病细胞分化和凋亡，具有抗炎活性。
TN1711	Gossypetin	Antioxidant; p38 MAPK; MAPK; Antibacterial	MAPK; Microbiology/Virology; oxidation-reduction
	Gossypetin 是一种可从Rhodiola rosea Linn.中提取的六羟基化的类黄酮，是一种有效的 MKK3 和 MKK6 抑制剂，可强烈减弱 MKK3/6-p38 信号传导途径。Gossypetin 具有抗突变、抗动脉粥样硬化、抗氧化以及细胞保护和抗菌作用，它通过下调溶酶体酪蛋白酶 K 的活性和诱导肌动蛋白环破骨细胞中的自噬相关蛋白来抑制骨吸收。
TN1484	Cheilanthifoline	NF-κB; Antifection	Microbiology/Virology; NF-κB
	Cheilanthifoline has anti-osteoclastogenic property, it gives significant inhibitions on receptor activator of nuclear factor-κB ligand-induced differentiation of mouse bone marrow-derived macrophages into multinucleated osteoclasts.
T37008	Reveromycin A
	Reveromycin A is the major component of a complex of spiroketal antibiotics isolated from Streptomyces sp. It inhibits the mitogenic activity of epidermal growth factor in Balb/MK cells (IC50 = 0.7 μg/ml), displays antiproliferative activity against human KB and K562 tumor cell lines (IC50s = 1.9 and 1.6 μg/ml, respectively), and demonstrates antifungal activity against C. albicans (MIC = 2 μg/ml at pH 3). Reveromycin A also has been shown to inhibit bone resorption by inducing apoptosis in oste...

天然产物

Cat.No: T3808

Synonym: 淫羊藿次苷I,Lcariside I,Icariin I,Icarisid I

Target: Others

Cat.No: T5770

Target: RANKL/RANK

Cat.No: T2789

Synonym: 黄岑素,野黄芩苷,Breviscapin,Breviscapinun,Breviscapine,Scutellarein-7-glucuronide

Target: Akt, HIV Protease, STAT

Cat.No: TN5888

Target: Others

Cat.No: TN1711

Target: Antioxidant, p38 MAPK, MAPK, Antibacterial

Cheilanthifoline

Cat.No: TN1484

Target: NF-κB, Antifection

Cat.No: T37008

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