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NE 10790

Catalog No. T16289 CAS 152831-36-2

Synonyms: 3-PEHPC

NE 10790 (3-PEHPC) is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak anti-resorptive agent. Although NE10790 was a poor inhibitor of FPP synthase

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NE 10790, CAS 152831-36-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 108.00
5 mg	In stock	$ 228.00
10 mg	In stock	$ 372.00
25 mg	In stock	$ 629.00
50 mg	In stock	$ 896.00
100 mg	In stock	$ 1,220.00

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Purity: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

NE 10790 (3-PEHPC) is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak anti-resorptive agent. Although NE10790 was a poor inhibitor of FPP synthase

In vitro

NE 10790 did inhibit prenylation in J774 macrophages and osteoclasts, but only of proteins of molecular mass approximately 22-26 kDa, the prenylation of which was not affected by peptidomimetic inhibitors of either farnesyl transferase (FTI-277) or geranylgeranyl transferase I (GGTI-298).?These 22-26-kDa proteins were shown to be geranylgeranylated by labelling J774 cells with [(3)H]geranylgeraniol.?Furthermore, NE10790 inhibited incorporation of [(14)C]mevalonic acid into Rab6, but not into H-Ras or Rap1, proteins that are modified by FTase and GGTase I, respectively.?These data demonstrate that NE10790 selectively prevents Rab prenylation in intact cells.?In accord, NE10790 inhibited the activity of recombinant Rab GGTase in vitro, but did not affect the activity of recombinant FTase or GGTase I. NE10790 therefore appears to be the first specific inhibitor of Rab GGTase to be identified.?In contrast to risedronate, NE10790 inhibited bone resorption in vitro without markedly affecting osteoclast number or the F-actin 'ring' structure in polarized osteoclasts.?However, NE10790 did alter osteoclast morphology, causing the formation of large intracellular vacuoles and protrusion of the basolateral membrane into large, 'domed' structures that lacked microvilli.?The anti-resorptive activity of NE10790 is thus likely due to disruption of Rab-dependent intracellular membrane trafficking in osteoclasts[1].

Synonyms	3-PEHPC
Molecular Weight	247.14
Formula	C8H10NO6P
CAS No.	152831-36-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 5 mg/mL (20.23 mM), when pH is adjusted to 6 with NaOH. Sonication is recommended.

DMSO: < 1mg/ml (insoluble）

References and Literature

1. Coxon FP, et al. Identification of a novel phosphonocarboxylate inhibitor of Rab geranylgeranyl transferase that specifically prevents Rab prenylation in osteoclasts and macrophages. J Biol Chem. 2001 Dec 21;276(51):48213-22. 2. Hald A , Hansen R R , Thomsen M W , et al. Cancer-induced bone loss and associated pain-related behavior is reduced by risedronate but not its phosphonocarboxylate analog NE-10790[J]. 2009, 125(5):1177-1185.

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Keywords

NE 10790 152831-36-2 Others inhibit 3-PEHPC NE10790 Inhibitor NE-10790 inhibitor

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