Art. -Nr.: HY-107720

ARL 17477

Name: ARL 17477
Brand: MedChemExpress
SKU: HY-107720
Price: 130.00 USD
Availability: InStock
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1 Cited Publications

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ARL 17477 is a blood-brain barrier-penetrant selective neuronal nitric oxide synthase (nNOS) inhibitor with an IC₅₀of 1 μM. ARL 17477 reduces nitric oxide production and activates TFEB and lysosomal biogenesis, induces lysosomal membrane permeabilization, but inhibits autophagy-lysosomal function, autophagic flux, protein aggregate clearance, and proliferation. ARL 17477 induces ERK hyperphosphorylation and slight AKT inhibition. ARL 17477 exhibits NOS1 -independent anticancer activity against multiple cancer cells. ARL 17477 inhibits xenograft tumor growth in vivo. ARL 17477 can be used in research on colon cancer, non-small cell lung cancer, osteosarcoma, pancreatic cancer, arterial occlusion, and pain.

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Reinheit : 98.88%
CAS. Nr.: 866914-87-6
Formel: C₂₀H₂₂Cl₃N₃S
Molecular Weight:442.83

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ARL 17477 Chemical Structure

CAS. Nr.: 866914-87-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

nNOS

1 μM (IC₅₀)

eNOS

17 μM (IC₅₀)

Alle NO Synthase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
SW48	IC50	15.0 μM	Cytotoxicity against human colon cancer SW48 cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay. Cytotoxicity against human colon cancer SW48 cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay.	37402770
U-251	IC50	13.0 μM	Cytotoxicity against human neuroblastoma U251-MG cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay. Cytotoxicity against human neuroblastoma U251-MG cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay.	37402770
HCT-116	IC50	7.4 μM	Cytotoxicity against human colon cancer HCT116 cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay. Cytotoxicity against human colon cancer HCT116 cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay.	37402770
A549	IC50	6.8 μM	Cytotoxicity against human lung cancer A549 cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay. Cytotoxicity against human lung cancer A549 cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay.	37402770
143B	IC50	4.4 μM	Cytotoxicity against human osteosarcoma 143B cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay. Cytotoxicity against human osteosarcoma 143B cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay.	37402770
MIA PaCa-2	IC50	4.3 μM	Cytotoxicity against human pancreatic cancer MIA PaCa-2 cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay. Cytotoxicity against human pancreatic cancer MIA PaCa-2 cells assessed as viability reduction incubated 2 days by Cell Counting Kit-8 assay.	37402770

In Vitro

ARL 17477 (2 days) inhibits the viability of SW48, U251-MG, HCT116, A549, 143B, MIA PaCa-2, and NOS1-/- U251-MG cells, with IC₅₀ values of 4.3-15.0 µM in the parental cell lines^[2].
ARL 17477 (7 days) inhibits TGS-01 glioblastoma CSC tumorsphere formation with an IC₅₀ of 4.4 µM^[2].
ARL 17477 (2 days) inhibits 143B-sph osteosarcoma CSC viability with an IC₅₀ of 1.1 µM^[2].
ARL 17477 (5-25 µM; 1 day) increases LC3B-II and p62, hyperphosphorylates ERK, and decreases full-length PARP without inducing caspase-3/PARP cleavage in U251-MG cells^[2].
ARL 17477 (25 µM; 48 h) activates lysosomal/TFEB and lipid synthesis gene programs in Panc-1 cells and suppresses the proliferation gene set^[2].
ARL 17477-induced intracellular accumulation of autophagy markers depends on impaired lysosomal acidification^[2].
ARL 17477 (1 µM; 30 min) inhibits lysosomal staining in MIA PaCa-2 cells^[2].
ARL 17477 (6 days) impairs protein aggregate clearance and increases aggregates in MIA PaCa-2 cells^[2].
ARL 17477 (100 µM; 1 h) induces lysosomal membrane permeabilization and increases cytosolic delivery in MIA PaCa-2 NanoBiT cells^[2].
ARL 17477 (60 min) is a selective inhibitor of recombinant human nNOS in the [3H]arginine to [3H]citrulline conversion assay (IC₅₀ = 1 μM), with weaker selectivity for eNOS (IC₅₀ = 17 μM)^[1].
ARL 17477 inhibits nNOS and endothelial NOS^[3].

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

Western Blot Analysis^[2]

Cell Line:

U251-MG neuroblastoma cells
Concentration:

5, 10, 25 µM
Incubation Time:

1 day; 6 h to 6 days (LC3B-II/p62)
Result:

Induced hyperphosphorylation of ERK with p-ERK/ERK band intensities of 1.0, 1.0, 1.3, and 4.1 at 0, 5, 10, and 25 µM.
Slightly suppressed AKT phosphorylation with p-AKT/AKT band intensities of 1.0, 1.0, 0.8, and 0.7.
Reduced full-length PARP.
Did not induce caspase-3 or PARP cleavage.
Increased p62 and LC3B-II protein levels.

In Vivo

ARL-17477 (10 mg/kg; i.v. tail vein bolus injection; daily; injection starts on day 14 after inoculation and ends on day 27) significantly delays tumor growth in the MIA PaCa-2 pancreatic cancer xenograft mouse model^[2].
ARL 17477 (10 mg/kg; i.p.; once daily; days 5-14 after stroke) improves post-stroke functional recovery on the rotarod task in wild-type C57Bl6 male mice with transient middle cerebral artery occlusion without altering infarct volume^[3].
ARL 17477 (0.4 mg/mL (0.9 mM); intraplantar injection; two prophylactic injections 15-20 minutes apart) does not prevent 7α,25-OHC (HY-113962)-induced mechanical allodynia in Sprague Dawley rats, but accelerates recovery to baseline within 96 hours^[4].

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

Animal Model:

BALB/c-nu/nu (female, 6 to 8-week-old)^[2]
Dosage:

10 mg/kg
Administration:

i.v. bolus via tail vein; daily; Injections started on day 14 after vaccination and ended on day 27
Result:

Significantly delayed tumor growth of MIA PaCa-2 xenografts compared with vehicle control.

Animal Model:

C57Bl6 (wild-type; male; 10-12 weeks old)^[3]
Dosage:

10 mg/kg
Administration:

i.p.; once daily each morning; post-stroke days 5-14
Result:

At post-stroke day 10, this compound-treated stroke mice exhibited functional improvement in rotating beam speed compared with vehicle-treated stroke mice.
Infarct area at the striatal and hippocampal levels and total infarct area did not differ between vehicle- and this compound-treated mice.

Animal Model:

Sprague Dawley (male and female, 200-250 g starting weight)^[4]
Dosage:

0.4 mg/mL (0.9 mM) in saline; 50 µL
Administration:

intraplantar; two prophylactic injections 15-20 minutes apart; first injection 15-20 minutes before 7α,25-OHC
Result:

Did not attenuate 7α,25-OHC-induced mechano-allodynia.
It began to accelerate recovery after 4 hours, with complete return to baseline by 96 hours.

Related Protocols :

Chemical Information

CAS. Nr. 866914-87-6
Appearance Solid
Molecular Weight 442.83
Formel C₂₀H₂₂Cl₃N₃S
Color Off-white to light yellow
SMILES

[H]Cl.[H]Cl.N=C(C1=CC=CS1)NC2=CC=C(CCNCC3=CC(Cl)=CC=C3)C=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (1)

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Journal Impact Factor

bioRxiv

Targeting GPR183 to reduce peripheral sensitization: evidence from rodent and human tissue analyses. [Abstract]

2026 Jan 16:2026.01.15.699745. PMID: 41648147

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 62.5 mg/mL (141.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 20 mg/mL (45.16 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2582 mL

11.2910 mL

22.5820 mL

5 mM

0.4516 mL

2.2582 mL

4.5164 mL

10 mM

0.2258 mL

1.1291 mL

2.2582 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. O'Neill MJ, et al. ARL 17477, a selective nitric oxide synthase inhibitor, with neuroprotective effects in animal models of global and focal cerebral ischaemia. Brain research. 2000 Jul 21;871(2):234-44.

[2]. Nomura TK, et al. ARL-17477 is a dual inhibitor of NOS1 and the autophagic-lysosomal system that prevents tumor growth in vitro and in vivo. Scientific reports. 2023 Jul 04;13(1):10757. [Content Brief]

[3]. Pendharkar AV, et al. Optogenetic Stimulation Reduces Neuronal Nitric Oxide Synthase Expression After Stroke. Translational stroke research. 2021 Apr;12(2):347-356.

[4]. Oberkrom K, et al. Targeting GPR183 to reduce peripheral sensitization: evidence from rodent and human tissue analyses. bioRxiv. 2026 Jan 16:2026-01. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.2582 mL	11.2910 mL	22.5820 mL	56.4551 mL
	5 mM	0.4516 mL	2.2582 mL	4.5164 mL	11.2910 mL
	10 mM	0.2258 mL	1.1291 mL	2.2582 mL	5.6455 mL
	15 mM	0.1505 mL	0.7527 mL	1.5055 mL	3.7637 mL
	20 mM	0.1129 mL	0.5646 mL	1.1291 mL	2.8228 mL
	25 mM	0.0903 mL	0.4516 mL	0.9033 mL	2.2582 mL
	30 mM	0.0753 mL	0.3764 mL	0.7527 mL	1.8818 mL
	40 mM	0.0565 mL	0.2823 mL	0.5646 mL	1.4114 mL
DMSO	50 mM	0.0452 mL	0.2258 mL	0.4516 mL	1.1291 mL
	60 mM	0.0376 mL	0.1882 mL	0.3764 mL	0.9409 mL
	80 mM	0.0282 mL	0.1411 mL	0.2823 mL	0.7057 mL
	100 mM	0.0226 mL	0.1129 mL	0.2258 mL	0.5646 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Bioz

ARL 17477

1 Cited Publications

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ARL 17477

Publications Citing Use of MedChemExpress (MCE) ARL 17477

Alle NO Synthase Isoform-spezifische Produkte anzeigen