1. Membrane Transporter/Ion Channel
  2. Chloride Channel
  3. ANO1-IN-5

ANO1-IN-5 is an orally active ANO1 inhibitor with an IC50 of 4.57 μM. J ANO1-IN-5 demonstrates 118-, 642-, and 10000-fold selectivity over α1A-1B-, andα1D-AR, respectively. ANO1-IN-5 exhibits significant inhibitory effects on osteoclast differentiation and function. ANO1-IN-5 can used for the study of osteoporosis.

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ANO1-IN-5

ANO1-IN-5 Chemical Structure

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Description

ANO1-IN-5 is an orally active ANO1 inhibitor with an IC50 of 4.57 μM. J ANO1-IN-5 demonstrates 118-, 642-, and 10000-fold selectivity over α1A-1B-, andα1D-AR, respectively. ANO1-IN-5 exhibits significant inhibitory effects on osteoclast differentiation and function. ANO1-IN-5 can used for the study of osteoporosis[1].

In Vitro

ANO1-IN-5 (Compound 10) (20 μM, 5 d) significantly inhibits the formation of TRAP+ multinucleated osteoclasts[1].
ANO1-IN-5 (20 μM) significantly reduces the mRNA expression of osteoclast marker genes such as NFATc1, Acp5, Ctsk, and Mmp9[1].
ANO1-IN-5 directly suppresses the Cl- secretion function of osteoclasts by inhibiting ANO1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. Tmax 0.083 h
Rat 10 mg/kg p.o. Tmax 4.00 h
Rat 1 mg/kg i.v. T1/2 1.62 h
Rat 10 mg/kg p.o. T1/2 2.76 h
Rat 1 mg/kg i.v. Cmax 2513 ng/mL
Rat 10 mg/kg p.o. Cmax 331.3 ng/mL
Rat 1 mg/kg i.v. AUC0-t 1520 ng·h/mL
Rat 10 mg/kg p.o. AUC0-t 2460 ng·h/mL
Rat 1 mg/kg i.v. AUC0-∞ 1520 ng·h/mL
Rat 10 mg/kg p.o. AUC0-∞ 2469 ng·h/mL
Rat 1 mg/kg i.v. ClF_obs 0.64 L/h/kg
Rat 10 mg/kg p.o. ClF_obs 4.11 L/kg
Rat 1 mg/kg i.v. Vz-F_obs 0.77 L/kg
Rat 10 mg/kg p.o. F 16.2 %
In Vivo

ANO1-IN-5 (Compound 10) (3-30 mg/kg, i.g., once daily for 4 weeks) effectively alleviates ovariectomy (OVX)-induced bone loss, significantly improving trabecular bone mass and morphological parameters in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: OVX-induced bone loss model established in 6-8-week-old female mice[1]
Dosage: 3, 10 and 30 mg/kg
Administration: Intragastrical administration (i.g.), once daily for 4 weeks
Result: Exhibited higher bone volume/total volume (BV/TV), trabecular number (Tb.N), and trabecular thickness (Tb.Th) values, but a lower trabecular separation (Tb.Sp) in a dose-dependent manner.
reduced the level of the bone resorption marker CTX-1 in the serum, and downregulated the expression of osteoclast marker genes in the bone tissue.
Molecular Weight

447.59

Formula

C23H33N3O4S

SMILES

O=S(C1=CC(CC(NC2CCN(C3=CC=CC=C3OCC)CC2)C)=CC=C1OC)(N)=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ANO1-IN-5
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HY-175669
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